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Jan Balzarini

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Ivana Perković; Sara Tršinar; Jelena Žanetić; Jan Balzarini; Dimitra Hadjipavlou-Litina; Anna-Maria Katsori; Marijeta Kralj; Irena Martin-Kleiner; Branka Zorc
Novel 1-acyl-4-substituted semicarbazide derivatives of primaquine - synthesis, cytostatic, antiviral and antioxidative studies.
Nadege Hamon; Jan Balzarini; Maurizio Quintiliani; Christopher McGuigan
Synthesis and biological evaluation of prodrugs of 2-fluoro-2-deoxyribose-1-phosphate and 2,2-difluoro-2-deoxyribose-1-phosphate.
Bart Hoorelbeke; Yasuhiro Igarashi; Patricia J LiWang; Rogier W Sanders; Haruo Tanaka; Els J M Van Damme; Thijs van Montfort; Jie Xue; Jan Balzarini
HIV-1 envelope trimer has similar binding characteristics for carbohydrate-binding agents as monomeric gp120.

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2013: Ivana Perković; Sara Tršinar; Jelena Žanetić; Jan Balzarini; Dimitra Hadjipavlou-Litina; Anna-Maria Katsori; Marijeta Kralj; Irena Martin-Kleiner; Branka Zorc
Novel 1-acyl-4-substituted semicarbazide derivatives of primaquine - synthesis, cytostatic, antiviral and antioxidative studies.
Journal of enzyme inhibition and medicinal chemistry 2013;28(3):601-10.
2013: Nadege Hamon; Jan Balzarini; Maurizio Quintiliani; Christopher McGuigan
Synthesis and biological evaluation of prodrugs of 2-fluoro-2-deoxyribose-1-phosphate and 2,2-difluoro-2-deoxyribose-1-phosphate.
Bioorganic & medicinal chemistry letters 2013;23(9):2555-9.
2013: Bart Hoorelbeke; Yasuhiro Igarashi; Patricia J LiWang; Rogier W Sanders; Haruo Tanaka; Els J M Van Damme; Thijs van Montfort; Jie Xue; Jan Balzarini
HIV-1 envelope trimer has similar binding characteristics for carbohydrate-binding agents as monomeric gp120.
FEBS letters 2013;587(7):860-6.
2013: Iwona E Głowacka; Jan Balzarini; Andrzej E Wróblewski
Synthesis and biological evaluation of novel 1,2,3-triazolonucleotides.
Archiv der Pharmazie 2013;346(4):278-91.
2013: Dongyue Li; Huiqing Liu; Jan Balzarini; Erik De Clercq; Christophe Pannecouque; Peng Zhan; Xinyong Liu
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
Bioorganic & medicinal chemistry 2013;21(7):2128-34.
2013: N Coen; Sophie Duraffour; U Singh; Robert Snoeck; Joost J van den Oord; V Vuyyuru; Jan Balzarini; Y C Cheng; C K Chu; Graciela Andrei
Activity and mechanism of action of HDVD, a novel pyrimidine nucleoside derivative with high levels of selectivity and potency against gammaherpesviruses.
Journal of virology 2013;87(7):3839-51.
2013: Silvia Meneghesso; Lieve Naesens; Evelien Vanderlinden; Jan Balzarini; Andrea Brancale; Christopher McGuigan
Synthesis and biological evaluation of purine 2'-fluoro-2'-deoxyriboside ProTides as anti-influenza virus agents.
ChemMedChem 2013;8(3):415-25.
2013: Kamil Kokosza; Jan Balzarini; Dorota G Piotrowska
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a carbamoyl linker.
Bioorganic & medicinal chemistry 2013;21(5):1097-108.
2013: Athina Dimopoulou; Dimitra-Niki Gkaragkouni; Christos Kiritsis; Stella Manta; IOANNIS PAPASOTIRIOU; Jan Balzarini; Dimitri Komiotis
Rapid microwave-enhanced synthesis of C5-alkynyl pyranonucleosides as novel cytotoxic antitumor agents.
Bioorganic & medicinal chemistry letters 2013;23(5):1330-3.
2013: Mikhail S Novikov; Christophe Pannecouque; Maria P Paramonova; Graciela Andrei; Denis A Babkov; Jan Balzarini; Sergey A Gavryushov; Alexander V Ivanov; Anastasiya Khandazhinskaya; Sergey N Kochetkov; Robert Snoeck; Vladimir T Valuev-Elliston; Katherine L Seley-Radtke
N1,N3-disubstituted uracils as nonnucleoside inhibitors of HIV-1 reverse transcriptase.
Bioorganic & medicinal chemistry 2013;21(5):1150-8.
2013: Rakesh Narang; Balasubramanian Narasimhan; Christophe Pannecouque; Sunil Sharma; Erik De Clercq; Jan Balzarini
Substituted naphthalen-1-yl-acetic acid hydrazides: synthesis, antimicrobial evaluation and QSAR analysis.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2013;9(2):249-74.
2013: Vikramjeet Judge; Balasubramanian Narasimhan; Christophe Pannecouque; Dharmarajan Sriram; Perumal Yogeeswari; Munish Ahuja; Erik De Clercq; Jan Balzarini
Synthesis, antimycobacterial, antiviral, antimicrobial activity and QSAR studies of N(2)-acyl isonicotinic acid hydrazide derivatives.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2013;9(1):53-76.
2012: Christos Kiritsis; Nikolaos Kollatos; Jan Balzarini; Athina Dimopoulou; Stella Manta; IOANNIS PAPASOTIRIOU; Vanessa Parmenopoulou; Dimitri Komiotis
Stereocontrolled synthesis of 4'-C-cyano and 4'-C-cyano-4'-deoxy pyrimidine pyranonucleosides as potential chemotherapeutic agents.
Carbohydrate research 2012;364():8-14.
2012: Marijke M F Alen; Jan Balzarini; Kai Dallmeier; Johan Neyts; Dominique Schols
Crucial role of the N-glycans on the viral E-envelope glycoprotein in DC-SIGN-mediated dengue virus infection.
Antiviral research 2012;96(3):280-7.
2012: Hiroki Kumamoto; Tomoko Miyaike; Tomohiko Nakano; Hiroshi Abe; Masanori Baba; Jan Balzarini; Kazuhiro Haraguchi; Mika Ito; Sachiko Kawahigashi; Yasuyuki Kitagawa; Hiromi Wakabayashi; Hiromichi Tanaka
Tuning efficiency of the 4-exo-trig cyclization by the electronic effect: ring closure of 3,3-difluoro-4-pentenyl carbon radicals and synthesis of a gem-difluorocyclobutane nucleoside.
Chemical communications (Cambridge, England) 2012;48(89):10993-5.
2012: Ugo Pradère; Vincent Roy; Ozkan Sari; Robert Snoeck; Graciela Andrei; Jan Balzarini; Manabu Hamada; Aurélien Montagu; Luigi A Agrofoglio
Synthesis and antiviral evaluation of bis(POM) prodrugs of (E)-[4'-phosphono-but-2'-en-1'-yl]purine nucleosides.
European journal of medicinal chemistry 2012;57():126-33.
2012: Christophe M Deroose; Rik Gijsbers; Abdelilah Ibrahimi; Veerle Baekelandt; Jan Balzarini; Guy Bormans; Satish K Chitneni; zeger debyser; Johan Nuyts; Alfons Verbruggen; Peter Vermaelen; Luc Mortelmans
Preliminary validation of varicella zoster virus thymidine kinase as a novel reporter gene for PET.
Nuclear medicine and biology 2012;39(8):1266-74.
2012: Geoffrey Férir; Dana Huskens; David M Markovitz; Kenneth Edward Palmer; Jan Balzarini; Daniel M Boudreaux; Michael D Swanson; Dominique Schols
Combinations of griffithsin with other carbohydrate-binding agents demonstrate superior activity against HIV Type 1, HIV Type 2, and selected carbohydrate-binding agent-resistant HIV Type 1 strains.
AIDS research and human retroviruses 2012;28(11):1513-23.
2012: Valentina D'Atri; Stefano D'Errico; haider shozeb; Bart Hoorelbeke; Luciano Mayol; Giorgia Oliviero; Jussara Amato; Jan Balzarini; Nicola Borbone; Vincenzo Piccialli; gennaro Piccialli
New anti-HIV aptamers based on tetra-end-linked DNA G-quadruplexes: effect of the base sequence on anti-HIV activity.
Chemical communications (Cambridge, England) 2012;48(76):9516-8.
2012: Jadd R Shelton; Jan Balzarini; Megan S Browning; Christopher Earl Cutler; Matt Peterson
Synthesis and SAR of 2',3'-bis-O-substituted N(6), 5'-bis-ureidoadenosine derivatives: implications for prodrug delivery and mechanism of action.
Bioorganic & medicinal chemistry letters 2012;22(19):6067-71.
2012: Xiao Li; Hong Liu; Huiqing Liu; Christophe Pannecouque; Liu Wang; Peng Zhan; Erik De Clercq; Jan Balzarini; Xuwang Chen; Dongyue Li; Xinyong Liu
Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.
Bioorganic & medicinal chemistry 2012;20(18):5527-36.
2012: Jie Xue; Bo Zhao; Jan Balzarini; Borries Demeler; Yongguang Gao; Bart Hoorelbeke; Ioannis Kagiampakis; Patricia J LiWang
The role of individual carbohydrate-binding sites in the function of the potent anti-HIV lectin griffithsin.
Molecular pharmaceutics 2012;9(9):2613-25.
2012: Alberto Diez-Torrubia; Jan Balzarini; Silvia Cabrera; María-José Camarasa; Ingrid De Meester; Sonsoles Velázquez
Dipeptidyl peptidase IV-activated prodrugs of anti-varicella zoster virus bicyclic nucleoside analogues containing different self-cleavage spacer systems.
ChemMedChem 2012;7(9):1612-22.
2012: Tomáš Tichý; Robert Snoeck; Graciela Andrei; Jan Balzarini; Martin Dračínský; Marcela Krecmerová
Synthesis and antiviral activities of hexadecyloxypropyl prodrugs of acyclic nucleoside phosphonates containing guanine or hypoxanthine and a (S)-HPMP or PEE acyclic moiety.
European journal of medicinal chemistry 2012;55():307-14.
2012: Jan Balzarini; Federico Gago; Anna Karlsson; Wim Kulik; Matt A Peterson; André B P van Kuilenburg; Morris J Robins
Introduction of a fluorine atom at C3 of 3-deazauridine shifts its antimetabolic activity from inhibition of CTP synthetase to inhibition of orotidylate decarboxylase, an early event in the de novo pyrimidine nucleotide biosynthesis pathway.
The Journal of biological chemistry 2012;287(36):30444-54.
2012: Edwuin H Rios Morales; Jan Balzarini; Chris Meier
Stereoselective synthesis and antiviral activity of methyl-substituted cycloSal-pronucleotides.
Journal of medicinal chemistry 2012;55(16):7245-52.
2012: Syed Shahzad-ul-Hussan; Jan Balzarini; Cajetan I Dogo-Isonagie; Rodolfo Ghirlando; Yasuhiro Igarashi; Carole A Bewley
Characterization and carbohydrate specificity of pradimicin S.
Journal of the American Chemical Society 2012;134(30):12346-9.
2012: Ekaterina A Khakina; Vyacheslav M Martynenko; Alexander V Mumyatov; Alexander S Peregudov; Sergey I Troyanov; Vyacheslav V Trush; Andrey I Vovk; Anastasiya A Yurkova; Jan Balzarini; pavel troshin
Highly selective reactions of C60Cl6 with thiols for the synthesis of functionalized [60]fullerene derivatives.
Chemical communications (Cambridge, England) 2012;48(57):7158-60.
2012: Mahesh K Lakshman; Robert Snoeck; Graciela Andrei; Raghavan Balachandran; Billy W Day; Amit Kumar; Jan Balzarini
Synthesis and biological properties of C-2 triazolylinosine derivatives.
The Journal of organic chemistry 2012;77(14):5870-83.
2012: Ozkan Sari; Robert Snoeck; Graciela Andrei; Jan Balzarini; Vincent Roy; Luigi A Agrofoglio
Synthesis and antiviral evaluation of C5-substituted-(1,3-diyne)-2'-deoxyuridines.
European journal of medicinal chemistry 2012;53():220-8.
2012: Shuang-Xi Gu; Qiu-Qin He; Zhi-Ming Li; Xiao-Dong Ma; Jan Balzarini; Fen-Er Chen; Erik De Clercq; Shi-Qiong Yang; Christophe Pannecouque
Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
European journal of medicinal chemistry 2012;53():229-34.
2012: Johan Vande Voorde; Kristof Vrancken; Federico Gago; Sandra Liekens; Jan Balzarini
Characterization of pyrimidine nucleoside phosphorylase of Mycoplasma hyorhinis: implications for the clinical efficacy of nucleoside analogues.
The Biochemical journal 2012;445(1):113-23.
2012: Karlo Wittine; Jan Balzarini; Sandra Kraljević Pavelić; Pieter Leyssen; Damjan Makuc; Johan Neyts; Krešimir Pavelić; Janez Plavec; Mirela Sedić; Maja Stipković Babić; Mladen Mintas
Novel 1,2,4-triazole and imidazole derivatives of L-ascorbic and imino-ascorbic acid: synthesis, anti-HCV and antitumor activity evaluations.
Bioorganic & medicinal chemistry 2012;20(11):3675-85.
2012: Kamaljit Singh; Jan Balzarini; Kelly Chibale; Hardeep Kaur; Susan Little; Prasad Bharatam
2-Aminopyrimidine based 4-aminoquinoline anti-plasmodial agents. Synthesis, biological activity, structure-activity relationship and mode of action studies.
European journal of medicinal chemistry 2012;52():82-97.
2012: Johan Vande Voorde; Sandra Liekens; Christopher McGuigan; Maurizio Quintiliani; Jan Balzarini
Inhibition of pyrimidine and purine nucleoside phosphorylases by a 3,5-dichlorobenzoyl-substituted 2-deoxy-D-ribose-1-phosphate derivative.
Biochemical pharmacology 2012;83(10):1358-63.
2012: Katrin Hartmann; D Klein; C Stengel; Herman F Egberink; Jan Balzarini
Efficacy and adverse effects of the antiviral compound plerixafor in feline immunodeficiency virus-infected cats.
Journal of veterinary internal medicine / American College of Veterinary Internal Medicine 2012;26(3):483-90.
2012: Christos Kiritsis; Jan Balzarini; Evdoxia Coutouli-Argyropoulou; Stella Manta; IOANNIS PAPASOTIRIOU; Sakellarios Trakossas; Dimitri Komiotis
Synthesis and biological evaluation of 3'-C-ethynyl and 3'-C-(1,4-disubstituted-1,2,3-triazolo) double-headed pyranonucleosides.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2012;8(3):320-9.
2012: Orrette R Wauchope; Robert Snoeck; Graciela Andrei; Jan Balzarini; Cameron Johnson; Pasupathy Krishnamoorthy; Katherine L Seley-Radtke
Synthesis and biological evaluation of a series of thieno-expanded tricyclic purine 2'-deoxy nucleoside analogues.
Bioorganic & medicinal chemistry 2012;20(9):3009-15.
2012: I Perković; Jan Balzarini; I Butula; Dimitra Hadjipavlou-Litina; Anna-Maria Katsori; Marijeta Kralj; I Martin-Kleiner; Branka Zorc
Novel NSAID 1-acyl-4-cycloalkyl/arylsemicarbazides and 1-acyl-5-benzyloxy/hydroxy carbamoylcarbazides as potential anticancer agents and antioxidants.
European journal of medicinal chemistry 2012;51():227-38.
2012: Xuwang Chen; Erik De Clercq; Christophe Pannecouque; Peng Zhan; Jan Balzarini; Xinyong Liu
Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
European journal of medicinal chemistry 2012;51():60-6.
2012: Christophe Vanpouille; Jan Balzarini; Marco Derudas; Jean-Charles Grivel; Andrea Introini; Andrea Lisco; Christopher McGuigan; Melanie Merbah; Arshi Munawwar; Ray F Schinazi; Leonid Margolis
Exploiting the anti-HIV-1 activity of acyclovir: suppression of primary and drug-resistant HIV isolates and potentiation of the activity by ribavirin.
Antimicrobial agents and chemotherapy 2012;56(5):2604-11.
2012: Iwona E Głowacka; Jan Balzarini; Andrzej E Wróblewski
Design, synthesis, antiviral, and cytotoxic evaluation of novel phosphonylated 1,2,3-triazoles as acyclic nucleotide analogues.
Nucleosides, nucleotides & nucleic acids 2012;31(4):293-318.
2012: Alberto Diez-Torrubia; Anne-Marie Lambeir; Jan Balzarini; Silvia Cabrera; María-José Camarasa; Sonsoles Velázquez
Dipeptidyl peptidase IV (DPPIV/CD26)-based prodrugs of hydroxy-containing drugs.
ChemMedChem 2012;7(4):618-28.
2012: Silvia Meneghesso; Jan Balzarini; Christopher McGuigan; Annelies Stevaert; Evelien Vanderlinden; Lieve Naesens
Synthesis and biological evaluation of pyrimidine nucleoside monophosphate prodrugs targeted against influenza virus.
Antiviral research 2012;94(1):35-43.
2012: Sandra Liekens; Beatrice Nico; Ghislain Opdenakker; María-Jesús Pérez-Pérez; Jan Balzarini; Mirella Belleri; Annelies Bronckaers; Antonella Bugatti; Elena Casanova; Alba Gigante; Domenico Ribatti; Rebecca Sienaert; Marco Presta
The thymidine phosphorylase inhibitor 5'-O-tritylinosine (KIN59) is an antiangiogenic multitarget fibroblast growth factor-2 antagonist.
Molecular cancer therapeutics 2012;11(4):817-29.
2012: Kathrin Reiser; Dominique Schols; Jan Balzarini; Tomas Bergman; Katrien O François; Hans Jörnvall; Anna Karlsson; Mathias Lundberg
Thioredoxin-1 and protein disulfide isomerase catalyze the reduction of similar disulfides in HIV gp120.
The international journal of biochemistry & cell biology 2012;44(3):556-62.
2012: Graciela Andrei; Jan Balzarini; Pierre Fiten; Christopher McGuigan; Ghislain Opdenakker; D Topalis; Robert Snoeck
In vitro-selected drug-resistant varicella-zoster virus mutants in the thymidine kinase and DNA polymerase genes yield novel phenotype-genotype associations and highlight differences between antiherpesvirus drugs.
Journal of virology 2012;86(5):2641-52.
2012: K O François; Jan Balzarini
Potential of carbohydrate-binding agents as therapeutics against enveloped viruses.
Medicinal research reviews 2012;32(2):349-87.
2012: Anja D Hartmann; Jan Balzarini; Natalie Wilhelm; Katrin Hartmann
Clinical efficacy of the acyclic nucleoside phosphonate 9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine (PMPDAP) in the treatment of feline immunodeficiency virus-infected cats.
Journal of feline medicine and surgery 2012;14(2):107-12.
2012: Jadd R Shelton; Jan Balzarini; Christopher Earl Cutler; Marcelio Oliveira; Matt A Peterson
Synthesis, SAR, and preliminary mechanistic evaluation of novel antiproliferative N⁶,5'-bis-ureido- and 5'-carbamoyl-N⁶-ureidoadenosine derivatives.
Bioorganic & medicinal chemistry 2012;20(2):1008-19.
2012: Thomas Vercruysse; Jan Balzarini; Beata Basta; François Debaene; Wim Dehaen; Nicolas Humbert; Yves Mély; Christophe Pannecouque; Sarah Sanglier-Cianférani; Dirk Daelemans
A phenyl-thiadiazolylidene-amine derivative ejects zinc from retroviral nucleocapsid zinc fingers and inactivates HIV virions.
Retrovirology 2012;9():95.
2012: Stella Manta; IOANNIS PAPASOTIRIOU; Vanessa Parmenopoulou; Jan Balzarini; Athina Dimopoulou; Christos Kiritsis; Nikolaos Kollatos; Dimitri Komiotis
Stereocontrolled facile synthesis and biological evaluation of (3'S) and (3'R)-3'-amino (and Azido)-3'-deoxy pyranonucleosides.
Nucleosides, nucleotides & nucleic acids 2012;31(7):522-35.
2012: Louise Egeblad; Staffan Eriksson; Susanne Flodin; Susanne Gräslund; Liya Wang; Martin Welin; Jan Balzarini; Pär Nordlund
Pan-pathway based interaction profiling of FDA-approved nucleoside and nucleobase analogs with enzymes of the human nucleotide metabolism.
PloS one 2012;7(5):e37724.
2012: Eva-María Priego; Jan Balzarini; María-José Camarasa; Federico Gago; Anna Karlsson; María-Jesús Pérez-Pérez
Recent advances in thymidine kinase 2 (TK2) inhibitors and new perspectives for potential applications.
Current pharmaceutical design 2012;18(20):2981-94.
2012: Sara Van Poecke; Davy Sinnaeve; Jan Balzarini; José C Martins; Serge Van Calenbergh
Synthesis of 5-substituted 2'-deoxyuridine-5'- phosphonate analogues and evaluation of their antiviral activity.
Nucleosides, nucleotides & nucleic acids 2012;31(3):256-72.
2012: Zeljka Babić; Jan Balzarini; Maja Crkvenčić; Marijeta Kralj; Ana-Matea Mikecin; Mariya Petrova; Zrinka Rajić; Jos Vanderleyden; Branka Zorc
New sorafenib derivatives: synthesis, antiproliferative activity against tumour cell lines and antimetabolic evaluation.
Molecules (Basel, Switzerland) 2012;17(1):1124-37.
2012: Jan Balzarini; Dominique Schols
Combination of antiretroviral drugs as microbicides.
Current HIV research 2012;10(1):53-60.
2012: Dorota G Piotrowska; Jan Balzarini; Iwona E Głowacka
Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a 1,2,3-triazole linker.
European journal of medicinal chemistry 2012;47(1):501-9.
2011: Xiao-Dong Ma; Shi-Qiong Yang; Jan Balzarini; Fen-Er Chen; Erik De Clercq; Shuang-Xi Gu; Qiu-Qin He; Christophe Pannecouque
Synthesis and anti-HIV activity of aryl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazones as potent non-nucleoside reverse transcriptase inhibitors.
ChemMedChem 2011;6(12):2225-32.
2011: Alamelu Mahalingam; Jan Balzarini; Anthony R Geonnotti; Patrick F Kiser
Activity and safety of synthetic lectins based on benzoboroxole-functionalized polymers for inhibition of HIV entry.
Molecular pharmaceutics 2011;8(6):2465-75.
2011: Shuang-Xi Gu; Qiu-Qin He; Xiao-Dong Ma; Jan Balzarini; Fen-Er Chen; Erik De Clercq; Hui-Fang Dai; Shi-Qiong Yang; Christophe Pannecouque
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
Bioorganic & medicinal chemistry 2011;19(23):7093-9.
2011: Romeo Romagnoli; Giampietro Viola; Su-zhan Zhang; Maria Kimatrai Salvador; Jun Li; LUISA-CARLOTA LÓPEZ-CARA; Jan Balzarini; Pier Giovanni Baraldi; Giuseppe Basso; Roberta Bortolozzi; Andrea Brancale; Xian-Hua Fu; Ernest Hamel
One-pot synthesis and biological evaluation of 2-pyrrolidinyl-4-amino-5-(3',4',5'-trimethoxybenzoyl)thiazole: a unique, highly active antimicrotubule agent.
European journal of medicinal chemistry 2011;46(12):6015-24.
2011: Ayşegül Karaküçük-İyidoğan; Emine Elçin Oruç-Emre; Demet Taşdemir; Jan Balzarini
Novel platinum(II) and palladium(II) complexes of thiosemicarbazones derived from 5-substitutedthiophene-2-carboxaldehydes and their antiviral and cytotoxic activities.
European journal of medicinal chemistry 2011;46(11):5616-24.
2011: Christos Kiritsis; Stella Manta; Vanessa Parmenopoulou; Jan Balzarini; Dimitri Komiotis
Branched-chain C-cyano pyranonucleosides: synthesis of 3'-C-cyano & 3'-C-cyano-3'-deoxy pyrimidine pyranonucleosides as novel cytotoxic agents.
European journal of medicinal chemistry 2011;46(11):5668-74.
2011: Christopher McGuigan; Paola Murziani; Magdalena Slusarczyk; Johan Vande Voorde; Blanka Gonczy; Sandra Liekens; Jan Balzarini
Phosphoramidate ProTides of the anticancer agent FUDR successfully deliver the preformed bioactive monophosphate in cells and confer advantage over the parent nucleoside.
Journal of medicinal chemistry 2011;54(20):7247-58.
2011: Graciela Andrei; Emanuela Balestra; Tomas Cihlar; Andrea Introini; Andrea Lisco; Leonid Margolis; Carlo Federico Perno; Robert Snoeck; Joost van den Oord; Christophe Vanpouille; Jan Balzarini
Topical tenofovir, a microbicide effective against HIV, inhibits herpes simplex virus-2 replication.
Cell host & microbe 2011;10(4):379-89.
2011: Swagatika Das; Umashankar Das; Erik De Clercq; Stephen G Dimmock; Dennis K J Gorecki; Carolina Lema; Armando Varela-Ramírez; Renato J Aguilera; Jan Balzarini; Jonathan R Dimmock
Bis[3,5-bis(benzylidene)-4-oxo-1-piperidinyl]amides: a novel class of potent cytotoxins.
ChemMedChem 2011;6(10):1892-9.
2011: Romeo Romagnoli; Jae Gwan Kim; Maria Kimatrai Salvador; LUISA-CARLOTA LÓPEZ-CARA; Antonio Ricci; Jan Balzarini; Pier Giovanni Baraldi; Jaime Bermejo; Andrea Brancale; Maria Dora Carrion; Longchuan Chen; Olga Cruz-Lopez; Francisco Estévez; Sara Estévez; Ernest Hamel
Synthesis and antitumor molecular mechanism of agents based on amino 2-(3',4',5'-trimethoxybenzoyl)benzo[b]furan: inhibition of tubulin and induction of apoptosis.
ChemMedChem 2011;6(10):1841-53.
2011: Mikhail S Novikov; Alexander A Ozerov; Christophe Pannecouque; Jan Balzarini; Galina V Gurskaya; Alexander V Ivanov; Olga N Ivanova; Sergey N Kochetkov; Kartik Temburnikar; Vladimir T Valuev-Elliston; Katherine L Seley-Radtke
1-[2-(2-Benzoyl- and 2-benzylphenoxy)ethyl]uracils as potent anti-HIV-1 agents.
Bioorganic & medicinal chemistry 2011;19(19):5794-802.
2011: Marina Moura; Elena Soriano; Albert Nguyen Van Nhien; Jan Balzarini; Sandrine Castelain; Gilles Duverlie; Carole Fournier; Solen Josse; José Marco-Contelles; Denis Postel
Synthesis and in vitro activity of novel N-3 acylated TSAO-T compounds against HIV-1 and HCV.
European journal of medicinal chemistry 2011;46(10):5046-56.
2011: María-Cruz Bonache; María-José Camarasa; Alessandra Cordeiro; Dirk Daelemans; Ernesto Quesada; Jan Balzarini; Els Vanstreels; Ana San-Félix
Selective inhibition of Human Immunodeficiency Virus type 1 (HIV-1) by a novel family of tricyclic nucleosides.
Antiviral research 2011;92(1):37-44.
2011: Shuang-Xi Gu; Qiu-Qin He; Xiao-Dong Ma; Jan Balzarini; Fen-Er Chen; Shi-Qiong Yang; Erik De Clercq; Christophe Pannecouque
Synthesis and structure-activity relationship of novel diarylpyrimidines with hydromethyl linker (CH(OH)-DAPYs) as HIV-1 NNRTIs.
Bioorganic & medicinal chemistry 2011;19(17):5117-24.
2011: Karine Barral; Bruno Canard; Céline Durafour; Johan Neyts; Nadine Payrot; Stéphane Priet; Loic Roux; Clément Weck; Fabien Zoulim; Jan Balzarini; Karine Alvarez
Acyclic nucleoside thiophosphonates as potent inhibitors of HIV and HBV replication.
European journal of medicinal chemistry 2011;46(9):4281-8.
2011: Yogesh Yadav; Erin D Maclean; Virinder S Parmar; Catherine K L Too; Jan Balzarini; Christopher J Barden; Annyt Bhattacharyya; Amitabh Jha
Design, synthesis and bioevaluation of novel candidate selective estrogen receptor modulators.
European journal of medicinal chemistry 2011;46(9):3858-66.
2011: Kiran S Toti; Jan Balzarini; Marco Derudas; Christopher McGuigan; Serge Van Calenbergh
Synthesis and antiviral evaluation of α-L-2'-deoxythreofuranosyl nucleosides.
European journal of medicinal chemistry 2011;46(9):3704-13.
2011: A G Bobylev; L G Bobyleva; D G Deryabin; R S Fadeev; I S Fadeeva; A B Kornev; Mila D Shpagina; pavel troshin; Jan Balzarini; Zoya A Podlubnaya
Fullerenolates: metallated polyhydroxylated fullerenes with potent anti-amyloid activity.
Organic & biomolecular chemistry 2011;9(16):5714-9.
2011: Virginia Lozano; Marleen Renders; Ana San-Félix; Dominique Schols; Leire Aguado; Jan Balzarini; María-José Camarasa; Bart Hoorelbeke; María-Jesús Pérez-Pérez
Targeting HIV entry through interaction with envelope glycoprotein 120 (gp120): synthesis and antiviral evaluation of 1,3,5-triazines with aromatic amino acids.
Journal of medicinal chemistry 2011;54(15):5335-48.
2011: Alexey B Kornev; Vyacheslav M Martynenko; Alexander S Peregudov; Jan Balzarini; Bart Hoorelbeke; pavel troshin
Synthesis and antiviral activity of highly water-soluble polycarboxylic derivatives of [70]fullerene.
Chemical communications (Cambridge, England) 2011;47(29):8298-300.
2011: Dana Hocková; Antonín Holý; Robert Snoeck; Graciela Andrei; Jan Balzarini
Acyclic nucleoside phosphonates with a branched 2-(2-phosphonoethoxy)ethyl chain: efficient synthesis and antiviral activity.
Bioorganic & medicinal chemistry 2011;19(15):4445-53.
2011: Maurizio Quintiliani; Robert Snoeck; Nicola Solaroli; Leentje Persoons; Graciela Andrei; Jan Balzarini; Anna Karlsson; Christopher McGuigan
Design, synthesis and biological evaluation of 2'-deoxy-2',2'-difluoro-5-halouridine phosphoramidate ProTides.
Bioorganic & medicinal chemistry 2011;19(14):4338-45.
2011: Tomáš Tichý; Graciela Andrei; Martin Dračínský; Antonín Holý; Jan Balzarini; Robert Snoeck; Marcela Krečmerová
New prodrugs of Adefovir and Cidofovir.
Bioorganic & medicinal chemistry 2011;19(11):3527-39.
2011: Geoffrey Férir; Kurt Vermeire; Dana Huskens; Jan Balzarini; Els J M Van Damme; Jan-Christoph Kehr; Elke Dittmann; Michael D Swanson; David M Markovitz; Dominique Schols
Synergistic in vitro anti-HIV type 1 activity of tenofovir with carbohydrate-binding agents (CBAs).
Antiviral research 2011;90(3):200-4.
2011: Bassam Al Atalah; Jan Balzarini; Nico Callewaert; Elke Fouquaert; Yi Lasanajak; Paul Proost; Pierre Rougé; David Smith; Dieter Vanderschaeghe; Els J M Van Damme
Expression analysis of the nucleocytoplasmic lectin 'Orysata' from rice in Pichia pastoris.
The FEBS journal 2011;278(12):2064-79.
2011: Kamaljit Singh; Kawaljit Singh; Baojie Wan; Scott Franzblau; Kelly Chibale; Jan Balzarini
Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity.
European journal of medicinal chemistry 2011;46(6):2290-4.
2011: André Bergman; Auke D Adema; Jan Balzarini; Skjalg Bruheim; Iduna Fichtner; Paul Noordhuis; Oystein Fodstad; F Myhren; ML Sandvold; HR Hendriks; Godefridus J Peters
Antiproliferative activity, mechanism of action and oral antitumor activity of CP-4126, a fatty acid derivative of gemcitabine, in in vitro and in vivo tumor models.
Investigational new drugs 2011;29(3):456-66.
2011: Umashankar Das; Hari N Pati; Hiroshi Sakagami; Ken Hashimoto; Masami Kawase; Jan Balzarini; Erik De Clercq; Jonathan R Dimmock
3,5-Bis(benzylidene)-1-[3-(2-hydroxyethylthio)propanoyl]piperidin-4-ones: a novel cluster of potent tumor-selective cytotoxins.
Journal of medicinal chemistry 2011;54(9):3445-9.
2011: Kristof Vrancken; Peter Vervaeke; Jan Balzarini; Sandra Liekens
Viruses as key regulators of angiogenesis.
Reviews in medical virology 2011;21(3):181-200.
2011: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Olga Cruz-Lopez; Manlio Tolomeo; Rosaria Maria Pipitone; Stefania Grimaudo; Jan Balzarini; Andrea Brancale; Antonietta Di Cristina; Ernest Hamel
Synthesis of novel antimitotic agents based on 2-amino-3-aroyl-5-(hetero)arylethynyl thiophene derivatives.
Bioorganic & medicinal chemistry letters 2011;21(9):2746-51.
2011: Kalyan Das; Chhaya Dharia; Angela S Rim; Jan Balzarini; Joseph D Bauman; María-José Camarasa; Arthur D Clark; Eddy Arnold
Crystal structure of tert-butyldimethylsilyl-spiroaminooxathioledioxide-thymine (TSAO-T) in complex with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket.
Journal of medicinal chemistry 2011;54(8):2727-37.
2011: Vaibhav P Mehta; Sachin G Modha; Eelco Ruijter; Kristof Van Hecke; Luc Van Meervelt; Christophe Pannecouque; Jan Balzarini; Romano V A Orru; Erik Van Der Eycken
A microwave-assisted diastereoselective multicomponent reaction to access dibenzo[c,e]azepinones: synthesis and biological evaluation.
The Journal of organic chemistry 2011;76(8):2828-39.
2011: Sonia De Castro; Olga Familiar; Graciela Andrei; Robert Snoeck; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
From β-amino-γ-sultone to unusual bicyclic pyridine and pyrazine heterocyclic systems: synthesis and cytostatic and antiviral activities.
ChemMedChem 2011;6(4):686-97.
2011: Ondřej Baszczyňski; Petr Jansa; Martin Dračínský; Blanka Klepetářová; Antonín Holý; Ivan Votruba; Erik de Clercq; Jan Balzarini; Zlatko Janeba
Synthesis and antiviral activity of N9-[3-fluoro-2-(phosphonomethoxy)propyl] analogues derived from N6-substituted adenines and 2,6-diaminopurines.
Bioorganic & medicinal chemistry 2011;19(7):2114-24.
2011: Niki Tzioumaki; Stella Manta; Evangelia Tsoukala; Sandra Liekens; Dimitri Komiotis; Johan Vande Voorde; Jan Balzarini
Synthesis and biological evaluation of unsaturated keto and exomethylene D-arabinopyranonucleoside analogs: novel 5-fluorouracil analogs that target thymidylate synthase.
European journal of medicinal chemistry 2011;46(4):993-1005.
2011: Giuseppe La Regina; Antonio Coluccia; Andrea Brancale; Francesco Piscitelli; Valerio Gatti; giovanni maga; Alberta Samuele; Christophe Pannecouque; Dominique Schols; Jan Balzarini; Ettore Novellino; Romano Silvestri
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide.
Journal of medicinal chemistry 2011;54(6):1587-98.
2011: Alberto Diez-Torrubia; Jan Balzarini; Graciela Andrei; Robert Snoeck; Ingrid De Meester; María-José Camarasa; Sonsoles Velázquez
Dipeptidyl peptidase IV dependent water-soluble prodrugs of highly lipophilic bicyclic nucleoside analogues.
Journal of medicinal chemistry 2011;54(6):1927-42.
2011: Thomas Vercruysse; Sonalika Pawar; Wim De Borggraeve; Els Pardon; George Pavlakis; Christophe Pannecouque; Jan Steyaert; Jan Balzarini; Dirk Daelemans
Measuring cooperative Rev protein-protein interactions on Rev responsive RNA by fluorescence resonance energy transfer.
RNA biology 2011;8(2):316-24.
2011: Giovanni Di Fabio; Jennifer D'Onofrio; Mariateresa Chiapparelli; Bart Hoorelbeke; Daniela Montesarchio; Jan Balzarini; Lorenzo De Napoli
Discovery of novel anti-HIV active G-quadruplex-forming oligonucleotides.
Chemical communications (Cambridge, England) 2011;47(8):2363-5.
2011: Sara Van Poecke; Ana Negri; Jolien Janssens; Nicola Solaroli; Anna Karlsson; Federico Gago; Jan Balzarini; Serge Van Calenbergh
Synthesis, modeling and evaluation of 3'-(1-aryl-1H-tetrazol-5-ylamino)-substituted 3'-deoxythymidine derivatives as potent and selective human mitochondrial thymidine kinase inhibitors.
Organic & biomolecular chemistry 2011;9(3):892-901.
2011: Edwuin H Rios Morales; Jan Balzarini; Chris Meier
Diastereoselective synthesis of cyclosaligenyl-nucleosyl-phosphotriesters.
Chemistry (Weinheim an der Bergstrasse, Germany) 2011;17(5):1649-59.
2011: Paula Pérez-Faginas; M Teresa Aranda; M Teresa García-López; Robert Snoeck; Graciela Andrei; Jan Balzarini; Rosario González-Muñiz
Synthesis and SAR studies on azetidine-containing dipeptides as HCMV inhibitors.
Bioorganic & medicinal chemistry 2011;19(3):1155-61.
2011: Aurélien Montagu; Vincent Roy; Jan Balzarini; Robert Snoeck; Graciela Andrei; Luigi A Agrofoglio
Synthesis of new C5-(1-substituted-1,2,3-triazol-4 or 5-yl)-2'-deoxyuridines and their antiviral evaluation.
European journal of medicinal chemistry 2011;46(2):778-86.
2011: Niki Tzioumaki; Evangelia Tsoukala; Stella Manta; Christos Kiritsis; Jan Balzarini; Dimitri Komiotis
Efficient synthesis of exomethylene- and keto-exomethylene-d-glucopyranosyl nucleoside analogs as potential cytotoxic agents.
Carbohydrate research 2011;346(2):328-33.
2011: Dimitri Topalis; Julie A C Alexandre; Graciela Andrei; Ahmed Azzouzi; Jan Balzarini; Julie Broggi; Christophe Caillat; Dominique Deville-Bonne; Chahrazade El-Amri; Staffan Eriksson; Jay Lin; Philippe Meyer; Ugo Pradère; Vincent Roy; Robert Snoeck; Luigi A Agrofoglio
Novel antiviral C5-substituted pyrimidine acyclic nucleoside phosphonates selected as human thymidylate kinase substrates.
Journal of medicinal chemistry 2011;54(1):222-32.
2011: Sebastien Debarge; Jan Balzarini; Anita R Maguire
Design and synthesis of α-carboxy phosphononucleosides.
The Journal of organic chemistry 2011;76(1):105-26.
2011: Davorka Završnik; Samija Muratović; Ante Nagl; Janez Plavec; Jan Balzarini; Mario Cetina; Erik De Clercq; Damjan Makuc; Mladen Mintas
Benzylidene-bis-(4-hydroxycoumarin) and benzopyrano-coumarin derivatives: synthesis, ¹H/¹³C-NMR conformational and X-ray crystal structure studies and in vitro antiviral activity evaluations.
Molecules (Basel, Switzerland) 2011;16(7):6023-40.
2011: Marijke M F Alen; Jan Balzarini; Tine De Burghgraeve; Suzanne J F Kaptein; Johan Neyts; Dominique Schols
Broad antiviral activity of carbohydrate-binding agents against the four serotypes of dengue virus in monocyte-derived dendritic cells.
PloS one 2011;6(6):e21658.
2011: Krešimir Benci; Leo Mandić; Jan Balzarini; Andrea Tomljenović Paravić; Krešimir Pavelić; Sandra Kraljević Pavelić; Tomislav Suhina; Karlo Wittine; Mladen Mintas
Novel 1,2,4-triazole and purine acyclic cyclopropane nucleoside analogues: synthesis, antiviral and cytostatic activity evaluations.
Antiviral chemistry & chemotherapy 2011;21(6):221-30.
2011: Michael Yee; Krystyna Konopka; Jan Balzarini; Nejat Düzgüneş
Inhibition of HIV-1 Env-Mediated Cell-Cell Fusion by Lectins, Peptide T-20, and Neutralizing Antibodies.
The open virology journal 2011;5():44-51.
2011: Bart Hoorelbeke; Els Jm Van Damme; Pierre Rougé; Dominique Schols; Kristel Van Laethem; Elke Fouquaert; Jan Balzarini
Differences in the mannose oligomer specificities of the closely related lectins from Galanthus nivalis and Zea mays strongly determine their eventual anti-HIV activity.
Retrovirology 2011;8(1):10.
2011: Katarzyna Kulik; Ewa Radzikowska; Renata Kaczmarek; Janina Baraniak; Wojciech J Stec; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Synthesis and an antiviral activity evaluation of nucleoside 5´-O-(N-acyl) phosphoramidates.
Antiviral chemistry & chemotherapy 2011;21(3):143-50.
2011: Paul Trippier; Jan Balzarini; Christopher McGuigan
Phenylboronic-acid-based carbohydrate binders as antiviral therapeutics: bisphenylboronic acids.
Antiviral chemistry & chemotherapy 2011;21(3):129-42.
2011: Andrey E Shchekotikhin; Valeria A Glazunova; Lyubov G Dezhenkova; Elena K Shevtsova; Valery F Traven'; Jan Balzarini; Hsu-Shan Huang; Alexander A Shtil; Maria N Preobrazhenskaya
The first series of 4,11-bis[(2-aminoethyl)amino]anthra[2,3-b]furan-5,10-diones: Synthesis and anti-proliferative characteristics.
European journal of medicinal chemistry 2011;46(1):423-8.
2010: Giorgia Oliviero; Jussara Amato; Nicola Borbone; Stefano D'Errico; Aldo Galeone; Luciano Mayol; haider shozeb; Olujide Olubiyi; Bart Hoorelbeke; Jan Balzarini; gennaro Piccialli
Tetra-end-linked oligonucleotides forming DNA G-quadruplexes: a new class of aptamers showing anti-HIV activity.
Chemical communications (Cambridge, England) 2010;46(47):8971-3.
2010: Snehlata Yadav; Pradeep Kumar; Erik De Clercq; Jan Balzarini; Christophe Pannecouque; Sharwan Kumar Dewan; Balasubramanian Narasimhan
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
European journal of medicinal chemistry 2010;45(12):5985-97.
2010: Evangelia Tsoukala; Niki Tzioumaki; Stella Manta; Alexandra Riga; Jan Balzarini; Dimitri Komiotis
Synthesis of 3-fluoro-6-S-(2-S-pyridyl) nucleosides as potential lead cytostatic agents.
Bioorganic chemistry 2010;38(6):285-93.
2010: Cristina Arbelo Roman; Jan Balzarini; Chris Meier
Diastereoselective synthesis of aryloxy phosphoramidate prodrugs of 3'-deoxy-2',3'-didehydrothymidine monophosphate.
Journal of medicinal chemistry 2010;53(21):7675-81.
2010: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Maria Giovanna Pavani; Olga Cruz-Lopez; Ernest Hamel; Jan Balzarini; Eleonora Brognara; Cristina Zuccato; Roberto Gambari
Synthesis and cellular pharmacology studies of a series of 2-amino-3-aroyl-4-substituted thiophene derivatives.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2010;6(6):329-43.
2010: Valentina Svicher; Claudia Alteri; Anna Artese; Federica Forbici; Maria Mercedes Santoro; Dominique Schols; Kristel Van Laethem; Stefano Alcaro; Giosuè Costa; Chiara Tommasi; Mauro Zaccarelli; Pasquale Narciso; Andrea Antinori; Francesca Ceccherini-Silberstein; Jan Balzarini; Carlo Federico Perno
Different evolution of genotypic resistance profiles to emtricitabine versus lamivudine in tenofovir-containing regimens.
Journal of acquired immune deficiency syndromes (1999) 2010;55(3):336-44.
2010: Sachin G Modha; Vaibhav P Mehta; Denis Ermolat'ev; Jan Balzarini; Kristof Van Hecke; Luc Van Meervelt; Erik Van Der Eycken
Microwave-assisted synthesis of a novel class of imidazolylthiazolidin-4-ones and evaluation of its biological activities.
Molecular diversity 2010;14(4):767-76.
2010: Marcela Krecmerová; Antonín Holý; Graciela Andrei; Karel Pomeisl; Tomás Tichý; Petra Brehová; Milena Masojídková; Martin Dracínský; Radek Pohl; Genevieve Laflamme; Lieve Naesens; Hon Hui; Tomas Cihlar; Johan Neyts; Erik De Clercq; Jan Balzarini; Robert Snoeck
Synthesis of ester prodrugs of 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-2,6-diaminopurine (HPMPDAP) as anti-poxvirus agents.
Journal of medicinal chemistry 2010;53(19):6825-37.
2010: Sandra Kraljević Pavelić; Mirela Sedić; Miroslav Poznić; Zrinka Rajić; Branka Zorc; Kresimir Pavelić; Jan Balzarini; Mladen Mintas
Evaluation of in vitro biological activity of O-alkylated hydroxamic derivatives of some nonsteroidal anti-inflammatory drugs.
Anticancer research 2010;30(10):3987-94.
2010: Dana Huskens; Geoffrey Férir; Kurt Vermeire; Jan-Christoph Kehr; Jan Balzarini; Elke Dittmann; Dominique Schols
Microvirin, a novel alpha(1,2)-mannose-specific lectin isolated from Microcystis aeruginosa, has anti-HIV-1 activity comparable with that of cyanovirin-N but a much higher safety profile.
The Journal of biological chemistry 2010;285(32):24845-54.
2010: Bart Hoorelbeke; Dana Huskens; Geoffrey Férir; Katrien O François; Atsushi Takahashi; Kristel Van Laethem; Dominique Schols; Haruo Tanaka; Jan Balzarini
Actinohivin, a broadly neutralizing prokaryotic lectin, inhibits HIV-1 infection by specifically targeting high-mannose-type glycans on the gp120 envelope.
Antimicrobial agents and chemotherapy 2010;54(8):3287-301.
2010: Lieselot Brepoels; Marijke De Saint-Hubert; Sigrid Stroobants; Gregor Verhoef; Jan Balzarini; Luc Mortelmans; Felix Mottaghy
Dose-response relationship in cyclophosphamide-treated B-cell lymphoma xenografts monitored with [18F]FDG PET.
European journal of nuclear medicine and molecular imaging 2010;37(9):1688-95.
2010: Sreekanth Thota; Subhas S Karki; K N Jayaveera; Jan Balzarini; Erik De Clercq
Synthesis, antineoplastic and cytotoxic activities of some mononuclear Ru(II) complexes.
Journal of enzyme inhibition and medicinal chemistry 2010;25(4):513-9.
2010: Zhao-Sen Zeng; Qiu-Qin He; Yong-Hong Liang; Xiao-Qing Feng; Fen-Er Chen; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
Bioorganic & medicinal chemistry 2010;18(14):5039-47.
2010: Hans P Steenackers; Jeremy Levin; Joost C Janssens; Ami De Weerdt; Jan Balzarini; Jos Vanderleyden; Dirk E De Vos; Sigrid C J De Keersmaecker
Structure-activity relationship of brominated 3-alkyl-5-methylene-2(5H)-furanones and alkylmaleic anhydrides as inhibitors of Salmonella biofilm formation and quorum sensing regulated bioluminescence in Vibrio harveyi.
Bioorganic & medicinal chemistry 2010;18(14):5224-33.
2010: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Maria Dora Carrion; Olga Cruz-Lopez; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Maria Rosaria Pipitone; Jan Balzarini; Andrea Brancale; Ernest Hamel
Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
Bioorganic & medicinal chemistry 2010;18(14):5114-22.
2010: Malina Jasamai; Claire Simons; Jan Balzarini
Synthesis of novel 6-azapyrimidine acyclic nucleoside analogues and antiviral evaluation.
Nucleosides, nucleotides & nucleic acids 2010;29(7):535-41.
2010: Yong-Hong Liang; Qiu-Qin He; Zhao-Sen Zeng; Zhi-Qian Liu; Xiao-Qing Feng; Fen-Er Chen; Jan Balzarini; Christophe Pannecouque; Erik De Clercq
Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry 2010;18(13):4601-5.
2010: Davinder Kumar; Vikramjeet Judge; Rakesh Narang; Sonia Sangwan; Erik De Clercq; Jan Balzarini; Balasubramanian Narasimhan
Benzylidene/2-chlorobenzylidene hydrazides: synthesis, antimicrobial activity, QSAR studies and antiviral evaluation.
European journal of medicinal chemistry 2010;45(7):2806-16.
2010: Zhao-Sen Zeng; Yong-Hong Liang; Xiao-Qing Feng; Fen-Er Chen; Christophe Pannecouque; Jan Balzarini; Erik De Clercq
Lead optimization of diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
ChemMedChem 2010;5(6):837-40.
2010: Kris Covens; Sarah Megens; Nathalie Dekeersmaeker; Kabamba Kabeya; Jan Balzarini; Stéphane De Wit; Anne-Mieke Vandamme; Kristel Van Laethem
The rare HIV-1 gp41 mutations 43T and 50V elevate enfuvirtide resistance levels of common enfuvirtide resistance mutations that did not impact susceptibility to sifuvirtide.
Antiviral research 2010;86(3):253-60.
2010: Romeo Romagnoli; Pier Giovanni Baraldi; Olga Cruz-Lopez; LUISA-CARLOTA LÓPEZ-CARA; Maria Dora Carrion; Jan Balzarini; Ernest Hamel; Giuseppe Basso; Roberta Bortolozzi; Giampietro Viola
Symmetrical alpha-bromoacryloylamido diaryldienone derivatives as a novel series of antiproliferative agents. Design, synthesis and biological evaluation.
Bioorganic & medicinal chemistry letters 2010;20(9):2733-9.
2010: Brian D Herman; Ivan Votruba; Antonin Holy; Nicolas Sluis-Cremer; Jan Balzarini
The acyclic 2,4-diaminopyrimidine nucleoside phosphonate acts as a purine mimetic in HIV-1 reverse transcriptase DNA polymerization.
The Journal of biological chemistry 2010;285(16):12101-8.
2010: Sara Van Poecke; Ana Negri; Federico Gago; Ineke Van Daele; Nicola Solaroli; Anna Karlsson; Jan Balzarini; Serge Van Calenbergh
3'-[4-Aryl-(1,2,3-triazol-1-yl)]-3'-deoxythymidine analogues as potent and selective inhibitors of human mitochondrial thymidine kinase.
Journal of medicinal chemistry 2010;53(7):2902-12.
2010: Xiao-Qing Feng; Zhao-Sen Zeng; Yong-Hong Liang; Fen-Er Chen; Christophe Pannecouque; Jan Balzarini; Erik De Clercq
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
Bioorganic & medicinal chemistry 2010;18(7):2370-4.
2010: Youcef Mehellou; Rocco Valente; Huw Mottram; Elisabeth Walsby; Kenneth I Mills; Jan Balzarini; Christopher McGuigan
Phosphoramidates of 2'-beta-D-arabinouridine (AraU) as phosphate prodrugs; design, synthesis, in vitro activity and metabolism.
Bioorganic & medicinal chemistry 2010;18(7):2439-46.
2010: Marco Derudas; Andrea Brancale; Lieve Naesens; Johan Neyts; Jan Balzarini; Christopher McGuigan
Application of the phosphoramidate ProTide approach to the antiviral drug ribavirin.
Bioorganic & medicinal chemistry 2010;18(7):2748-55.
2010: Jan Balzarini; Katrien O François; Kristel Van Laethem; Bart Hoorelbeke; Marleen Renders; Joeri Auwerx; Sandra Liekens; Toshikazu Oki; Yasuhiro Igarashi; Dominique Schols
Pradimicin S, a highly soluble nonpeptidic small-size carbohydrate-binding antibiotic, is an anti-HIV drug lead for both microbicidal and systemic use.
Antimicrobial agents and chemotherapy 2010;54(4):1425-35.
2010: Stella Manta; Evangelia Tsoukala; Niki Tzioumaki; Christos Kiritsis; Jan Balzarini; Dimitri Komiotis
Synthesis of 4,6-dideoxy-3-fluoro-2-keto-beta-D-glucopyranosyl analogues of 5-fluorouracil, N6-benzoyl adenine, uracil, thymine, N4-benzoyl cytosine and evaluation of their antitumor activities.
Bioorganic chemistry 2010;38(2):48-55.
2010: Amitabh Jha; Chandrani Mukherjee; Ashok K Prasad; Virinder S Parmar; Manjula Vadaparti; Umashankar Das; Erik De Clercq; Jan Balzarini; James P Stables; Anuraag Shrivastav; Rajendra K Sharma; Jonathan R Dimmock
Derivatives of aryl amines containing the cytotoxic 1,4-dioxo-2-butenyl pharmacophore.
Bioorganic & medicinal chemistry letters 2010;20(5):1510-5.
2010: Ramendra K Singh; Diwakar Rai; Dipti Yadav; A Bhargava; Jan Balzarini; Erik De Clercq
Synthesis, antibacterial and antiviral properties of curcumin bioconjugates bearing dipeptide, fatty acids and folic acid.
European journal of medicinal chemistry 2010;45(3):1078-86.
2010: Christophe Vanpouille; Andrea Lisco; Marco Derudas; Elisa Saba; Jean-Charles Grivel; Beda Brichacek; Francesca Scrimieri; Ray F Schinazi; Dominique Schols; Christopher McGuigan; Jan Balzarini; Leonid Margolis
A new class of dual-targeted antivirals: monophosphorylated acyclovir prodrug derivatives suppress both human immunodeficiency virus type 1 and herpes simplex virus type 2.
The Journal of infectious diseases 2010;201(4):635-43.
2010: Karine Barral; Stéphane Priet; Céline De Michelis; Joséphine Sire; Johan Neyts; Jan Balzarini; Bruno Canard; Karine Alvarez
Synthesis and antiviral activity of boranophosphonate isosteres of AZT and d4T monophosphates.
European journal of medicinal chemistry 2010;45(2):849-56.
2010: Jean-Jacques Bosc; Laurent Latxague; Jean-Michel Léger; Jan Balzarini; Isabelle Forfar; Christian Jarry; Jean Guillon
Synthesis and in vitro cytostatic activity of new beta-D-arabino furan[1',2':4,5]oxazolo- and arabino-pyrimidinone derivatives.
European journal of medicinal chemistry 2010;45(2):831-9.
2010: Alberto Diez-Torrubia; Carlos García-Aparicio; Silvia Cabrera; Ingrid De Meester; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
Application of the dipeptidyl peptidase IV (DPPIV/CD26) based prodrug approach to different amine-containing drugs.
Journal of medicinal chemistry 2010;53(2):559-72.
2010: I Ozturk; S Filimonova; Sotiris K Hadjikakou; Nikolaos Kourkoumelis; V Dokorou; Manolis J Manos; Anastasios J Tasiopoulos; M M Barsan; Ian S Butler; E R Milaeva; Jan Balzarini; Nick Hadjiliadis
Structural motifs and biological studies of new antimony(III) iodide complexes with thiones.
Inorganic chemistry 2010;49(2):488-501.
2010: Marco Derudas; Maurizio Quintiliani; Andrea Brancale; Graciela Andrei; Robert Snoeck; Jan Balzarini; Christopher McGuigan
Evaluation of novel phosphoramidate ProTides of the 2'-fluoro derivatives of a potent anti-varicella zoster virus bicyclic nucleoside analogue.
Antiviral chemistry & chemotherapy 2010;21(1):15-31.
2010: Paul Trippier; Christopher McGuigan; Jan Balzarini
Phenylboronic-acid-based carbohydrate binders as antiviral therapeutics: monophenylboronic acids.
Antiviral chemistry & chemotherapy 2010;20(6):249-57.
2010: Mohammad-Ali Jenabian; Héla Saïdi; Charlotte Charpentier; Hicham Bouhlal; Dominique Schols; Jan Balzarini; Thomas W Bell; Guido Vanham; Laurent Bélec
Differential activity of candidate microbicides against early steps of HIV-1 infection upon complement virus opsonization.
AIDS research and therapy 2010;7():16.
2010: Mia Bjerke; Nicola Solaroli; Nicole Lesko; Jan Balzarini; Magnus Johansson; Anna Karlsson
Retained sensitivity to cytotoxic pyrimidine nucleoside analogs in thymidine kinase 2 deficient human fibroblasts.
Nucleosides, nucleotides & nucleic acids 2010;29(1):1-13.
2010: Youcef Mehellou; Jan Balzarini; Christopher McGuigan
The design, synthesis and antiviral evaluation of a series of 5-trimethylsilyl-1-beta-D-(arabinofuranosyl)uracil phosphoramidate ProTides.
Antiviral chemistry & chemotherapy 2010;20(4):153-60.
2010: Thierry Huet; Olivier Kerbarh; Dominique Schols; Pascal Clayette; Cécile Gauchet; Guy Dubreucq; Loïc Vincent; Heidi Bompais; Romain Mazinghien; Olivier Querolle; Arnaud Salvador; Jérôme Lemoine; Bruno Lucidi; Jan Balzarini; Maurice Petitou
Long-lasting enfuvirtide carrier pentasaccharide conjugates with potent anti-human immunodeficiency virus type 1 activity.
Antimicrobial agents and chemotherapy 2010;54(1):134-42.
2009: Subhas S Karki; Rahul Hazare; Sujeet Kumar; Vivek S Bhadauria; Jan Balzarini; Erik De Clercq
Synthesis, anticancer and cytostatic activity of some 6H-indolo[2,3-b]quinoxalines.
Acta pharmaceutica (Zagreb, Croatia) 2009;59(4):431-40.
2009: Mohammad-Ali Jenabian; Héla Saïdi; Charlotte Charpentier; Yven Van Herrewege; Jong Chan Son; Dominique Schols; Jan Balzarini; Guido Vanham; Laurent Bélec
In vitro synergistic activity against CCR5-tropic HIV-1 with combinations of potential candidate microbicide molecules HHA, KRV2110 and enfuvirtide (T20).
The Journal of antimicrobial chemotherapy 2009;64(6):1192-5.
2009: Christopher McGuigan; Marco Derudas; Maurizio Quintiliani; Graciela Andrei; Robert Snoeck; Geoffrey Henson; Jan Balzarini
2'-Fluorosugar analogues of the highly potent anti-varicella-zoster virus bicyclic nucleoside analogue (BCNA) Cf 1743.
Bioorganic & medicinal chemistry letters 2009;19(22):6264-7.
2009: Dani Youssef; Elizabeth Potter; Mamta Jha; Erik De Clercq; Jan Balzarini; James P Stables; Amitabh Jha
Design, synthesis and bioevaluation of novel maleamic amino acid ester conjugates of 3,5-bisarylmethylene-4-piperidones as cytostatic agents.
Bioorganic & medicinal chemistry letters 2009;19(22):6364-7.
2009: Swagatika Das; Umashankar Das; Ponniah Selvakumar; Rajendra K Sharma; Jan Balzarini; Erik De Clercq; Joseph Molnár; Julianna Serly; Zoltán Baráth; Gabriele Schatte; Brian Bandy; Dennis K J Gorecki; Jonathan R Dimmock
3,5-Bis(benzylidene)-4-oxo-1-phosphonopiperidines and related diethyl esters: Potent cytotoxins with multi-drug-resistance reverting properties.
ChemMedChem 2009;4(11):1831-40.
2009: Youcef Mehellou; Jan Balzarini; Christopher McGuigan
Aryloxy phosphoramidate triesters: a technology for delivering monophosphorylated nucleosides and sugars into cells.
ChemMedChem 2009;4(11):1779-91.
2009: Katrien O François; Christophe Pannecouque; Joeri Auwerx; Virginia Lozano; María-Jesús Pérez-Pérez; Dominique Schols; Jan Balzarini
The phthalocyanine prototype derivative Alcian Blue is the first synthetic agent with selective anti-human immunodeficiency virus activity due to its gp120 glycan-binding potential.
Antimicrobial agents and chemotherapy 2009;53(11):4852-9.
2009: Stella Manta; Niki Tzioumaki; Evangelia Tsoukala; Aggeliki Panagiotopoulou; Maria Pelecanou; Jan Balzarini; Dimitri Komiotis
Unsaturated dideoxy fluoro-ketopyranosyl nucleosides as new cytostatic agents: a convenient synthesis of 2,6-dideoxy-3-fluoro-4-keto-beta-D-glucopyranosyl analogues of uracil, 5-fluorouracil, thymine, N4-benzoyl cytosine and N6-benzoyl adenine.
European journal of medicinal chemistry 2009;44(11):4764-71.
2009: Annelies Bronckaers; Federico Gago; Jan Balzarini; Sandra Liekens
The dual role of thymidine phosphorylase in cancer development and chemotherapy.
Medicinal research reviews 2009;29(6):903-53.
2009: Constance Auvynet; Dimitri Topalis; Christophe Caillat; Hélène Munier-Lehmann; Edward Seclaman; Jan Balzarini; Luigi A Agrofoglio; Pierre Alexandre Kaminski; Philippe Meyer; Dominique Deville-Bonne; Chahrazade El Amri
Phosphorylation of dGMP analogs by vaccinia virus TMP kinase and human GMP kinase.
Biochemical and biophysical research communications 2009;388(1):6-11.
2009: Deepika Sharma; Balasubramanian Narasimhan; Pradeep Kumar; Vikramjeet Judge; Rakesh Narang; Erik De Clercq; Jan Balzarini
Synthesis, antimicrobial and antiviral activity of substituted benzimidazoles.
Journal of enzyme inhibition and medicinal chemistry 2009;24(5):1161-8.
2009: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Maria Dora Carrion; Carlota Lopez Cara; Olga Cruz-Lopez; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Maria Rosaria Pipitone; Jan Balzarini; Nicola Zonta; Andrea Brancale; Ernest Hamel
Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
Bioorganic & medicinal chemistry 2009;17(19):6862-71.
2009: Christopher McGuigan; Jan Balzarini
FV100 as a new approach for the possible treatment of varicella-zoster virus infection.
The Journal of antimicrobial chemotherapy 2009;64(4):671-3.
2009: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; Maria Dora Carrion; Olga Cruz-Lopez; Carlota Lopez Cara; Giuseppe Basso; Giampietro Viola; Mohammed Khedr; Jan Balzarini; Siavosh Mahboobi; Andreas Sellmer; Andrea Brancale; Ernest Hamel
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization.
Journal of medicinal chemistry 2009;52(17):5551-5.
2009: Marco Derudas; Davide Carta; Andrea Brancale; Christophe Vanpouille; Andrea Lisco; Leonid Margolis; Jan Balzarini; Christopher McGuigan
The application of phosphoramidate protide technology to acyclovir confers anti-HIV inhibition.
Journal of medicinal chemistry 2009;52(17):5520-30.
2009: Sophie Curbo; Magnus Johansson; Jan Balzarini; Lionel D Lewis; Anna Karlsson
Acute cytotoxicity of arabinofuranosyl nucleoside analogs is not dependent on mitochondrial DNA.
Experimental cell research 2009;315(15):2539-43.
2009: Yong-Hong Liang; Xiao-Qing Feng; Zhao-Sen Zeng; Fen-Er Chen; Jan Balzarini; Christophe Pannecouque; Erik De Clercq
Design, synthesis, and SAR of naphthyl-substituted Diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
ChemMedChem 2009;4(9):1537-45.
2009: Osama I el-Sabbagh; Mohamed M Baraka; Samy M Ibrahim; Christophe Pannecouque; Graciela Andrei; Robert Snoeck; Jan Balzarini; Adel AHMED Rashad
Synthesis and antiviral activity of new pyrazole and thiazole derivatives.
European journal of medicinal chemistry 2009;44(9):3746-53.
2009: Egor P Tchesnokov; Aleksandr Obikhod; Ivana Massud; Andrea Lisco; Christophe Vanpouille; Beda Brichacek; Jan Balzarini; Christopher McGuigan; Marco Derudas; Leonid Margolis; Ray F Schinazi; Matthias Götte
Mechanisms associated with HIV-1 resistance to acyclovir by the V75I mutation in reverse transcriptase.
The Journal of biological chemistry 2009;284(32):21496-504.
2009: A Bronckaers; L Aguado; A Negri; María-José Camarasa; Jan Balzarini; María-Jesús Pérez-Pérez; F Gago; S Liekens
Identification of aspartic acid-203 in human thymidine phosphorylase as an important residue for both catalysis and non-competitive inhibition by the small molecule "crystallization chaperone" 5'-O-tritylinosine (KIN59).
Biochemical pharmacology 2009;78(3):231-40.
2009: Anna N Tevyashova; Eugenia N Olsufyeva; Konstantin F Turchin; Jan Balzarini; Eugenyi E Bykov; Lyubov G Dezhenkova; Alexander A Shtil; Maria N Preobrazhenskaya
Reaction of the antitumor antibiotic olivomycin I with aryl diazonium salts. Synthesis, cytotoxic and antiretroviral potency of 5-aryldiazenyl-6-O-deglycosyl derivatives of olivomycin I.
Bioorganic & medicinal chemistry 2009;17(14):4961-7.
2009: Joeri Auwerx; Katrien O François; Els Vanstreels; Kristel Van Laethem; Dirk Daelemans; Dominique Schols; Jan Balzarini
Capture and transmission of HIV-1 by the C-type lectin L-SIGN (DC-SIGNR) is inhibited by carbohydrate-binding agents and polyanions.
Antiviral research 2009;83(1):61-70.
2009: Youcef Mehellou; Jan Balzarini; Christopher McGuigan
An investigation into the anti-HIV activity of 2',3'-didehydro-2',3'-dideoxyuridine (d4U) and 2',3'-dideoxyuridine (ddU) phosphoramidate 'ProTide' derivatives.
Organic & biomolecular chemistry 2009;7(12):2548-53.
2009: Nicolas Gisch; Jan Balzarini; Chris Meier
Doubly loaded cycloSaligenyl-pronucleotides - 5,5'-Bis-(cycloSaligenyl-2',3'-dideoxy-2',3'-didehydrothymidine monophosphates).
Journal of medicinal chemistry 2009;52(11):3464-73.
2009: Sandra Liekens; Annelies Bronckaers; Jan Balzarini
Improvement of purine and pyrimidine antimetabolite-based anticancer treatment by selective suppression of mycoplasma-encoded catabolic enzymes.
The lancet oncology 2009;10(6):628-35.
2009: Niki Tzioumaki; Evangelia Tsoukala; Stella Manta; George Agelis; Jan Balzarini; Dimitri Komiotis
Synthesis, antiviral and cytostatic evaluation of unsaturated exomethylene and keto D-lyxopyranonucleoside analogues.
Archiv der Pharmazie 2009;342(6):353-60.
2009: Mariola Koszytkowska-Stawińska; Erik De Clercq; Jan Balzarini
Synthesis and antiviral activity evaluation of acyclic 2'-azanucleosides bearing a phosphonomethoxy function in the side chain.
Bioorganic & medicinal chemistry 2009;17(11):3756-62.
2009: Umashankar Das; Hari N Pati; Atulya K Panda; Erik De Clercq; Jan Balzarini; Joseph Molnár; Zoltán Baráth; Imre Ocsovszki; Masami Kawase; Li Zhou; Hiroshi Sakagami; Jonathan R Dimmock
2-(3-Aryl-2-propenoyl)-3-methylquinoxaline-1,4-dioxides: a novel cluster of tumor-specific cytotoxins which reverse multidrug resistance.
Bioorganic & medicinal chemistry 2009;17(11):3909-15.
2009: Stella Manta; Evangelia Tsoukala; Niki Tzioumaki; Ales Goropevsek; Ravi Teja Pamulapati; Avrelija Cencic; Jan Balzarini; Dimitri Komiotis
Dideoxy fluoro-ketopyranosyl nucleosides as potent antiviral agents: synthesis and biological evaluation of 2,3- and 3,4-dideoxy-3-fluoro-4- and -2-keto-beta-d-glucopyranosyl derivatives of N(4)-benzoyl cytosine.
European journal of medicinal chemistry 2009;44(6):2696-704.
2009: Bo Liu; Hao Peng; Qing Yao; Jing Li; Els Van Damme; Jan Balzarini; Jin-Ku Bao
Bioinformatics analyses of the mannose-binding lectins from Polygonatum cyrtonema, Ophiopogon japonicus and Liparis noversa with antiproliferative and apoptosis-inducing activities.
Phytomedicine : international journal of phytotherapy and phytopharmacology 2009;16(6-7):601-8.
2009: Joeri Auwerx; Ola Isacsson; Johan Söderlund; Jan Balzarini; Magnus Johansson; Mathias Lundberg
Human glutaredoxin-1 catalyzes the reduction of HIV-1 gp120 and CD4 disulfides and its inhibition reduces HIV-1 replication.
The international journal of biochemistry & cell biology 2009;41(6):1269-75.
2009: Deepika Sharma; Balasubramanian Narasimhan; Pradeep Kumar; Vikramjeet Judge; Rakesh Narang; Erik De Clercq; Jan Balzarini
Synthesis, antimicrobial and antiviral evaluation of substituted imidazole derivatives.
European journal of medicinal chemistry 2009;44(6):2347-53.
2009: Morris J Robins; Hong Yang; Karl Miranda; Matt Peterson; Erik De Clercq; Jan Balzarini
Synthesis and biological evaluation of 3,3-difluoropyridine-2,4(1H,3H)-dione and 3-deaza-3-fluorouracil base and nucleoside derivatives.
Journal of medicinal chemistry 2009;52(9):3018-27.
2009: Jan Balzarini; Ineke Van Daele; Ana Negri; Nicola Solaroli; Anna Karlsson; Sandra Liekens; Federico Gago; Serge Van Calenbergh
Human mitochondrial thymidine kinase is selectively inhibited by 3'-thiourea derivatives of beta-thymidine: identification of residues crucial for both inhibition and catalytic activity.
Molecular pharmacology 2009;75(5):1127-36.
2009: Marijke M F Alen; Suzanne J F Kaptein; Tine De Burghgraeve; Jan Balzarini; Johan Neyts; Dominique Schols
Antiviral activity of carbohydrate-binding agents and the role of DC-SIGN in dengue virus infection.
Virology 2009;387(1):67-75.
2009: Christopher McGuigan; Olivier Bidet; Marco Derudas; Graciela Andrei; Robert Snoeck; Jan Balzarini
Alkenyl substituted bicyclic nucleoside analogues retain nanomolar potency against Varicella Zoster Virus.
Bioorganic & medicinal chemistry 2009;17(8):3025-7.
2009: Francesco Piscitelli; Antonio Coluccia; Andrea Brancale; Giuseppe La Regina; Anna Sansone; Cesare Giordano; Jan Balzarini; giovanni maga; Samantha Zanoli; Alberta Samuele; Roberto Cirilli; Francesco La Torre; Antonio Lavecchia; Ettore Novellino; Romano Silvestri
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
Journal of medicinal chemistry 2009;52(7):1922-34.
2009: Yuan-Zhen Xiong; Fen-Er Chen; Jan Balzarini; Erik De Clercq; Christophe Pannecouque
Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 13: synthesis of fluorine-containing diaryltriazine derivatives for in vitro anti-HIV evaluation against wild-type strain.
Chemistry & biodiversity 2009;6(4):561-8.
2009: Romeo Romagnoli; Pier Giovanni Baraldi; Maria Dora Carrion; Olga Cruz-Lopez; LUISA-CARLOTA LÓPEZ-CARA; Jan Balzarini; Ernest Hamel; Alessandro Canella; Enrica Fabbri; Roberto Gambari; Giuseppe Basso; Giampietro Viola
Hybrid alpha-bromoacryloylamido chalcones. Design, synthesis and biological evaluation.
Bioorganic & medicinal chemistry letters 2009;19(7):2022-8.
2009: Subhas S Karki; Vivek Singh Bahaduria; Vivek Rana; Sujeet Kumar; Prasanna G Subbaro; Umashankar Das; Jan Balzarini; Erik De Clercq; Jonathan R Dimmock
1-Arylmethyl-2,3-dioxo-2,3-dihydroindole thiosemicarbazones as leads for developing cytotoxins and anticonvulsants.
Journal of enzyme inhibition and medicinal chemistry 2009;24(2):537-44.
2009: Sonia De Castro; Carlos García-Aparicio; Graciela Andrei; Robert Snoeck; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
4-Benzyloxy-gamma-sultone derivatives: discovery of a novel family of non-nucleoside inhibitors of human cytomegalovirus and varicella zoster virus.
Journal of medicinal chemistry 2009;52(6):1582-91.
2009: Elke Fouquaert; David Smith; Willy J Peumans; Paul Proost; Jan Balzarini; Savvas N Savvides; Els J M Van Damme
Related lectins from snowdrop and maize differ in their carbohydrate-binding specificity.
Biochemical and biophysical research communications 2009;380(2):260-5.
2009: Ibrahim I Ozturk; Sotiris K Hadjikakou; Nick Hadjiliadis; Nikolaos Kourkoumelis; Maciej Kubicki; Anastasios J Tasiopoulos; Hanadi Scleiman; Mirela M Barsan; Ian S Butler; Jan Balzarini
New antimony(III) bromide complexes with thioamides: synthesis, characterization, and cytostatic properties.
Inorganic chemistry 2009;48(5):2233-45.
2009: Andrey E Shchekotikhin; Valeria A Glazunova; Lyubov G Dezhenkova; Yuri N Luzikov; Yuri B Sinkevich; Leonid V Kovalenko; Vladimir N Buyanov; Jan Balzarini; Fong-Chun Huang; Jing-Jer Lin; Hsu-Shan Huang; Alexander A Shtil; Maria N Preobrazhenskaya
Synthesis and cytotoxic properties of 4,11-bis[(aminoethyl)amino]anthra[2,3-b]thiophene-5,10-diones, novel analogues of antitumor anthracene-9,10-diones.
Bioorganic & medicinal chemistry 2009;17(5):1861-9.
2009: Z Rajic; Ivan Butula; Branka Zorc; Sandra Kraljevic Pavelic; Karlo Hock; Kresimir Pavelic; Lieve Naesens; Erik De Clercq; Jan Balzarini; Monika Przyborowska; Tadeusz Ossowski; Mladen Mintas
Cytostatic and antiviral activity evaluations of hydroxamic derivatives of some non-steroidal anti-inflammatory drugs.
Chemical biology & drug design 2009;73(3):328-38.
2009: Hui Lv; Yang Kong; Qing Yao; Bo Zhang; Fang-Wei Leng; He-Jiao Bian; Jan Balzarini; Els Van Damme; Jin-Ku Bao
Nebrodeolysin, a novel hemolytic protein from mushroom Pleurotus nebrodensis with apoptosis-inducing and anti-HIV-1 effects.
Phytomedicine : international journal of phytotherapy and phytopharmacology 2009;16(2-3):198-205.
2009: Yue-Ping Wang; Fen-Er Chen; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Synthesis and in vitro anti-HIV evaluation of a new series of 6-arylmethyl-substituted S-DABOs as potential non-nucleoside HIV-1 reverse transcriptase inhibitors.
European journal of medicinal chemistry 2009;44(3):1016-23.
2009: Cristina Chamorro; John A W Kruijtzer; Marina Farsaraki; Jan Balzarini; Rob M J Liskamp
A general approach for the non-stop solid phase synthesis of TAC-scaffolded loops towards protein mimics containing discontinuous epitopes.
Chemical communications (Cambridge, England) 2009;(7):821-3.
2009: Yuan-Zhen Xiong; Hai-Rong Hu; Fen-Er Chen; Jan Balzarini; Christophe Pannecouque; Erik De Clercq
Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.
Yao xue xue bao = Acta pharmaceutica Sinica 2009;44(2):145-9.
2009: Xiao-Qing Feng; Yong-Hong Liang; Zhao-Sen Zeng; Fen-Er Chen; Jan Balzarini; Christophe Pannecouque; Erik De Clercq
Structural modifications of DAPY analogues with potent anti-HIV-1 activity.
ChemMedChem 2009;4(2):219-24.
2009: Kazuhiro Haraguchi; Hisashi Shimada; Genta Akutsu; Keigo Kimura; Hiromichi Tanaka; Takayuki Hamasaki; Masanori Baba; Elizabeth A Gullen; Ginger E Dutschman; Yung-Chi Cheng; Jan Balzarini
Synthesis and anti-HIV activity of 4'-C-ethynyl-2'-deoxy-4'-thio-nucleosides.
Nucleic acids symposium series (2004) 2009;(53):97-8.
2009: Philippe Meyer; Christophe Caillat; Dimitri Topalis; Jan Balzarini; Dominique Deville-Bonne
Structural basis for the specificity of thymidylate kinases from human pathogens: implications for nucleotide analogues activation.
Nucleic acids symposium series (2004) 2009;(53):41.
2009: Yutaka Kubota; Nobuhide Ishizaki; Yuri Kaneda; Kazuhiro Haraguchi; Yuki Odanaka; Hiromichi Tanaka; Nobuyuki Kato; Masanori Baba; Jan Balzarini
Synthesis and antiviral evaluation of 4'-alkoxy analogues of 9-(beta-D-xylofuranosyl)adenine.
Antiviral chemistry & chemotherapy 2009;19(5):201-12.
2009: Samir Abdurahman; Ákos Végvári; Michael Levi; Stefan Höglund; Marita Högberg; Weimin Tong; Ivan Romero; Jan Balzarini; Anders Vahlne
Isolation and characterization of a small antiretroviral molecule affecting HIV-1 capsid morphology.
Retrovirology 2009;6():34.
2009: Anna N Tevyashova; Eugenia N Olsufyeva; Eugenia N Zbarsky; Jan Balzarini; Alexander A Shtil; Lyubov G Dezhenkova; Vladimir M Bukhman; Victor B Zbarsky; Maria N Preobrazhenskaya
Modification of the antibiotic olivomycin I at the 2'-keto group of the side chain. Novel derivatives, antitumor and topoisomerase I-poisoning activity.
The Journal of antibiotics 2009;62(1):37-41.
2009: K Wittine; K Benci; Z Rajić; Branka Zorc; Marijeta Kralj; M Marjanović; K Pavelić; Erik De Clercq; Graciela Andrei; Robert Snoeck; Jan Balzarini; Mladen Mintas
The novel phosphoramidate derivatives of NSAID 3-hydroxypropylamides: synthesis, cytostatic and antiviral activity evaluations.
European journal of medicinal chemistry 2009;44(1):143-51.
2009: Hari N Pati; Umashankar Das; Swagatika Das; Brian Bandy; Erik De Clercq; Jan Balzarini; Masami Kawase; Hiroshi Sakagami; J Wilson Quail; James P Stables; Jonathan R Dimmock
The cytotoxic properties and preferential toxicity to tumour cells displayed by some 2,4-bis(benzylidene)-8-methyl-8-azabicyclo[3.2.1] octan-3-ones and 3,5-bis(benzylidene)-1-methyl-4-piperidones.
European journal of medicinal chemistry 2009;44(1):54-62.
2009: Jan Balzarini; Barbara Orzeszko-Krzesińska; Jan K Maurin; Andrzej Orzeszko
Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones.
European journal of medicinal chemistry 2009;44(1):303-11.
2008: Joeri Auwerx; Katrien O François; Kris Covens; Kristel Van Laethem; Jan Balzarini
Glycan deletions in the HIV-1 gp120 V1/V2 domain compromise viral infectivity, sensitize the mutant virus strains to carbohydrate-binding agents and represent a specific target for therapeutic intervention.
Virology 2008;382(1):10-9.
2008: Nicolas Gisch; Jan Balzarini; Chris Meier
Studies on enzyme-cleavable dialkoxymethyl-cyclosaligenyl-2',3'-dideoxy-2',3'-didehydrothymidine monophosphates.
Journal of medicinal chemistry 2008;51(21):6752-60.
2008: Christophe Caillat; Dimitri Topalis; Luigi A Agrofoglio; Sylvie Pochet; Jan Balzarini; Dominique Deville-Bonne; Philippe Meyer
Crystal structure of poxvirus thymidylate kinase: an unexpected dimerization has implications for antiviral therapy.
Proceedings of the National Academy of Sciences of the United States of America 2008;105(44):16900-5.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Taradas Sarkar; LUISA-CARLOTA LÓPEZ-CARA; Olga Cruz Lopez; Maria Dora Carrion; Delia Preti; Manlio Tolomeo; Jan Balzarini; Ernest Hamel
Synthesis and biological evaluation of 2-aroyl-4-phenyl-5-hydroxybenzofurans as a new class of antitubulin agents.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2008;4(6):558-64.
2008: Henning J Jessen; Jan Balzarini; Chris Meier
Intracellular trapping of cycloSal-pronucleotides: modification of prodrugs with amino acid esters.
Journal of medicinal chemistry 2008;51(20):6592-8.
2008: Samir Abdurahman; Ákos Végvári; Masoud Youssefi; Michael Levi; Stefan Höglund; Elin Andersson; Peter Horal; Bo Svennerholm; Jan Balzarini; Anders Vahlne
Activity of the small modified amino acid alpha-hydroxy glycineamide on in vitro and in vivo human immunodeficiency virus type 1 capsid assembly and infectivity.
Antimicrobial agents and chemotherapy 2008;52(10):3737-44.
2008: Sonia De Castro; M Teresa Peromingo; Lieve Naesens; Graciela Andrei; Robert Snoeck; Jan Balzarini; Sonsoles Velázquez; María-José Camarasa
4"-Benzoylureido-TSAO derivatives as potent and selective non-nucleoside HCMV inhibitors. Structure-activity relationship and mechanism of antiviral action.
Journal of medicinal chemistry 2008;51(18):5823-32.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Taradas Sarkar; Maria Dora Carrion; Olga Cruz-Lopez; LUISA-CARLOTA LÓPEZ-CARA; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Maria Rosaria Pipitone; Jan Balzarini; Roberto Gambari; Lampronti Ilaria; Roberto Saletti; Andrea Brancale; Ernest Hamel
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
Bioorganic & medicinal chemistry 2008;16(18):8419-26.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Maria Dora Carrion; Olga Cruz-Lopez; LUISA-CARLOTA LÓPEZ-CARA; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Maria Rosa Pipitone; Jan Balzarini; Sahar Kandil; Andrea Brancale; Taradas Sarkar; Ernest Hamel
Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
Bioorganic & medicinal chemistry letters 2008;18(18):5041-5.
2008: Andrea Lisco; Christophe Vanpouille; Egor P Tchesnokov; Jean-Charles Grivel; Angélique Biancotto; Beda Brichacek; Julie Elliott; Emilie Fromentin; Robin J Shattock; Peter A Anton; Robert J Gorelick; Jan Balzarini; Christopher McGuigan; Marco Derudas; Matthias Götte; Ray F Schinazi; Leonid Margolis
Acyclovir is activated into a HIV-1 reverse transcriptase inhibitor in herpesvirus-infected human tissues.
Cell host & microbe 2008;4(3):260-70.
2008: Oriana Tabarrini; Serena Massari; Dirk Daelemans; Miguel Stevens; Giuseppe Manfroni; Stefano Sabatini; Jan Balzarini; Violetta Cecchetti; Christophe Pannecouque; Arnaldo Fravolini
Structure-activity relationship study on anti-HIV 6-desfluoroquinolones.
Journal of medicinal chemistry 2008;51(17):5454-8.
2008: María-Jesús Pérez-Pérez; Eva-María Priego; Ana-Isabel Hernández; Olga Familiar; María-José Camarasa; Ana Negri; Federico Gago; Jan Balzarini
Structure, physiological role, and specific inhibitors of human thymidine kinase 2 (TK2): present and future.
Medicinal research reviews 2008;28(5):797-820.
2008: Christopher McGuigan; Marco Derudas; Joachim Bugert; Graciela Andrei; Robert Snoeck; Jan Balzarini
Successful kinase bypass with new acyclovir phosphoramidate prodrugs.
Bioorganic & medicinal chemistry letters 2008;18(15):4364-7.
2008: Emanuela Balestrieri; Arianna Ascolani; Yasuhiro Igarashi; Toshikazu Oki; Antonio Mastino; Jan Balzarini; Beatrice Macchi
Inhibition of cell-to-cell transmission of human T-cell lymphotropic virus type 1 in vitro by carbohydrate-binding agents.
Antimicrobial agents and chemotherapy 2008;52(8):2771-9.
2008: Katrien O François; Joeri Auwerx; Dominique Schols; Jan Balzarini
Simian immunodeficiency virus is susceptible to inhibition by carbohydrate-binding agents in a manner similar to that of HIV: implications for further preclinical drug development.
Molecular pharmacology 2008;74(2):330-7.
2008: Nicola Solaroli; Magnus Johansson; L Persoons; Jan Balzarini; Anna Karlsson
Substrate specificity of feline and canine herpesvirus thymidine kinase.
Antiviral research 2008;79(2):128-32.
2008: Béatrice Gerland; Jérôme Désiré; Jan Balzarini; Jean-Luc Décout
Anti-retroviral and cytostatic activity of 2',3'-dideoxyribonucleoside 3'-disulfides.
Bioorganic & medicinal chemistry 2008;16(14):6824-31.
2008: Annelies Bronckaers; Jan Balzarini; Sandra Liekens
The cytostatic activity of pyrimidine nucleosides is strongly modulated by Mycoplasma hyorhinis infection: Implications for cancer therapy.
Biochemical pharmacology 2008;76(2):188-97.
2008: M Bjerke; Jan Balzarini; Anna Karlsson
Reduced levels of mitochondrial DNA increases the toxicity of 9-beta-D-arabinofuranosylguanine (araG).
Nucleosides, nucleotides & nucleic acids 2008;27(6):746-9.
2008: Nikolaos Lougiakis; Panagiotis Marakos; Nicole Pouli; Nicole Poul; Jan Balzarini
Synthesis and antiviral activity evaluation of some novel acyclic C-nucleosides.
Chemical & pharmaceutical bulletin 2008;56(6):775-80.
2008: Umashankar Das; Alireza Doroudi; Swagatika Das; Brian Bandy; Jan Balzarini; Erik De Clercq; Jonathan R Dimmock
E,E-2-Benzylidene-6-(nitrobenzylidene)cyclohexanones: syntheses, cytotoxicity and an examination of some of their electronic, steric, and hydrophobic properties.
Bioorganic & medicinal chemistry 2008;16(11):6261-8.
2008: Ivana Perković; Ivan Butula; Branka Zorc; Karlo Hock; Sandra Kraljević Pavelić; Kresimir Pavelić; Erik De Clercq; Jan Balzarini; Mladen Mintas
Novel lipophilic hydroxyurea derivatives: synthesis, cytostatic and antiviral activity evaluations.
Chemical biology & drug design 2008;71(6):546-53.
2008: Yuan-Zhen Xiong; Fen-Er Chen; Jan Balzarini; Erik De Clercq; Christophe Pannecouque
Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: structural modulations of diaryltriazines with potent anti-HIV activity.
European journal of medicinal chemistry 2008;43(6):1230-6.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Olga Cruz-Lopez; Delia Preti; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Nicola Zonta; Jan Balzarini; Andrea Brancale; Taradas Sarkar; Ernest Hamel
Design, synthesis, and biological evaluation of thiophene analogues of chalcones.
Bioorganic & medicinal chemistry 2008;16(10):5367-76.
2008: Tatjana Gazivoda; Silvana Raić-Malić; Vedran Kristafor; Damjan Makuc; Janez Plavec; Sinisa Bratulić; Sandra Kraljević-Pavelić; Kresimir Pavelić; Lieve Naesens; Graciela Andrei; Robert Snoeck; Jan Balzarini; Mladen Mintas
Synthesis, cytostatic and anti-HIV evaluations of the new unsaturated acyclic C-5 pyrimidine nucleoside analogues.
Bioorganic & medicinal chemistry 2008;16(10):5624-34.
2008: Hari N Pati; Umashankar Das; Masami Kawase; Hiroshi Sakagami; Jan Balzarini; Erik De Clercq; Jonathan R Dimmock
1-Aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides and related adducts: A quest for selective cytotoxicity for malignant cells.
Bioorganic & medicinal chemistry 2008;16(10):5747-53.
2008: Cyrille Tomassi; Albert Nguyen Van Nhien; José Marco-Contelles; Jan Balzarini; Christophe Pannecouque; Erik De Clercq; Denis Postel
Synthesis and anti-HIV1 biological activity of novel 5''-ATSAO compounds.
Bioorganic & medicinal chemistry 2008;16(8):4733-41.
2008: María-Cruz Bonache; Ernesto Quesada; Chih-Wei Sheen; Jan Balzarini; Nicolas Sluis-Cremer; María-Jesús Pérez-Pérez; María-José Camarasa; Ana San-Félix
Novel N-3 substituted TSAO-T derivatives: synthesis and anti-HIV-evaluation.
Nucleosides, nucleotides & nucleic acids 2008;27(4):351-67.
2008: Cyrille Tomassi; Van Nhien Albert Nguyen; José Marco-Contelles; Jan Balzarini; Christophe Pannecouque; Erik De Clercq; Elena Soriano; Denis Postel
Synthesis, anti-HIV-1 activity, and modeling studies of N-3 Boc TSAO compound.
Bioorganic & medicinal chemistry letters 2008;18(7):2277-81.
2008: Yue-Ping Wang; Fen-Er Chen; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry 2008;16(7):3887-94.
2008: Pal Perjesi; Umashankar Das; Erik De Clercq; Jan Balzarini; Masame Kawase; Hiroshi Sakagami; James P Stables; Tamas Lorand; Zsuzsanna Rozmer; Jonathan R Dimmock
Design, synthesis and antiproliferative activity of some 3-benzylidene-2,3-dihydro-1-benzopyran-4-ones which display selective toxicity for malignant cells.
European journal of medicinal chemistry 2008;43(4):839-45.
2008: Mia Bjerke; Maribel Franco; Magnus Johansson; Jan Balzarini; Anna Karlsson
Increased mitochondrial DNA copy-number in CEM cells resistant to delayed toxicity of 2',3'-dideoxycytidine.
Biochemical pharmacology 2008;75(6):1313-21.
2008: Romeo Romagnoli; Pier Giovanni Baraldi; Taradas Sarkar; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Olga Cruz-Lopez; Delia Preti; Mojgan Aghazadeh Tabrizi; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Nicola Zonta; Jan Balzarini; Andrea Brancale; Hsing-Pang Hsieh; Ernest Hamel
Synthesis and biological evaluation of 1-methyl-2-(3',4',5'-trimethoxybenzoyl)-3-aminoindoles as a new class of antimitotic agents and tubulin inhibitors.
Journal of medicinal chemistry 2008;51(5):1464-8.
2008: Jennifer D'Onofrio; Luigi Petraccone; Luigi Martino; Giovanni Di Fabio; Alfonso Iadonisi; Jan Balzarini; Concetta Giancola; Daniela Montesarchio
Synthesis, biophysical characterization, and anti-HIV activity of glyco-conjugated G-quadruplex-forming oligonucleotides.
Bioconjugate chemistry 2008;19(3):607-16.
2008: Malina Jasamai; Jan Balzarini; Claire Simons
6-Azathymidine-4'-thionucleosides: synthesis and antiviral evaluation.
Journal of enzyme inhibition and medicinal chemistry 2008;23(1):56-61.
2008: Michela Pollicita; Dominique Schols; Stefano Aquaro; W J Peumans; E J M Van Damme; Carlo Federico Perno; Jan Balzarini
Carbohydrate-binding agents (CBAs) inhibit HIV-1 infection in human primary monocyte-derived macrophages (MDMs) and efficiently prevent MDM-directed viral capture and subsequent transmission to CD4+ T lymphocytes.
Virology 2008;370(2):382-91.
2008: Henning Jacob Jessen; Tilmann Schulz; Jan Balzarini; Chris Meier
Bioreversible protection of nucleoside diphosphates.
Angewandte Chemie (International ed. in English) 2008;47(45):8719-22.
2008: Diwakar Rai; Dipti Yadav; Jan Balzarini; Erik De Clercq; Ramendra K Singh
Design and development of curcumin bioconjugates as antiviral agents.
Nucleic acids symposium series (2004) 2008;(52):599-600.
2008: Dipti Yadav; Diwakar Rai; Jan Balzarini; Erik De Clercq; Ramendra K Singh
Thymidine analogs as potential antiviral agents.
Nucleic acids symposium series (2004) 2008;(52):263-4.
2008: Chris Meier; H J Jessen; Jan Balzarini
Nucleoside diphosphate prodrugs.
Nucleic acids symposium series (2004) 2008;(52):83-4.
2008: Dana Huskens; Kurt Vermeire; Elise Vandemeulebroucke; Jan Balzarini; Dominique Schols
Safety concerns for the potential use of cyanovirin-N as a microbicidal anti-HIV agent.
The international journal of biochemistry & cell biology 2008;40(12):2802-14.
2008: Yueping Wang; Fen-Er Chen; Jan Balzarini; Erik De Clercq; Christophe Pannecouque
Non-nucleoside HIV-1 reverse-transcriptase inhibitors. Part 10. Synthesis and anti-HIV activity of 5-alkyl-6-(1-naphthylmethyl)pyrimidin-4(3H)-ones with a mono- or disubstituted 2-amino function as novel 'dihydro-alkoxy-benzyl-oxopyrimidine' (DABO) analogues.
Chemistry & biodiversity 2008;5(1):168-76.
2007: Marco D Migliore; Nicola Zonta; Christopher McGuigan; Geoffrey Henson; Graciela Andrei; Robert Snoeck; Jan Balzarini
Synthesis and antiviral activity of the carbocyclic analogue of the highly potent and selective anti-VZV bicyclo furano pyrimidines.
Journal of medicinal chemistry 2007;50(26):6485-92.
2007: Satish K Chitneni; Christophe M Deroose; Jan Balzarini; Rik Gijsbers; Sofie Celen; zeger debyser; Luc Mortelmans; Alfons Verbruggen; Guy Bormans
A p-[18F]fluoroethoxyphenyl bicyclic nucleoside analogue as a potential positron emission tomography imaging agent for varicella-zoster virus thymidine kinase gene expression.
Journal of medicinal chemistry 2007;50(26):6627-37.
2007: Sandra Liekens; Annelies Bronckaers; María-Jesús Pérez-Pérez; Jan Balzarini
Targeting platelet-derived endothelial cell growth factor/thymidine phosphorylase for cancer therapy.
Biochemical pharmacology 2007;74(11):1555-67.
2007: Christopher McGuigan; Ranjith N Pathirana; Marco Migliore; Rina Adak; Giovanna M Luoni; Arwyn T Jones; Alberto Díez-Torrubia; Maria-Jose Camarasa; Sonsoles Velázquez; Geoffrey Henson; Erik Verbeken; Rebecca Sienaert; Lieve Naesens; Robert Snoeck; Graciela Andrei; Jan Balzarini
Preclinical development of bicyclic nucleoside analogues as potent and selective inhibitors of varicella zoster virus.
The Journal of antimicrobial chemotherapy 2007;60(6):1316-30.
2007: Khalid El Akri; Khalid Bougrin; Jan Balzarini; Abdesslem Faraj; Rachid Benhida
Efficient synthesis and in vitro cytostatic activity of 4-substituted triazolyl-nucleosides.
Bioorganic & medicinal chemistry letters 2007;17(23):6656-9.
2007: Nicola Solaroli; Xinyu Zheng; Magnus Johansson; Jan Balzarini; Anna Karlsson
Mitochondrial expression of the Drosophila melanogaster multisubstrate deoxyribonucleoside kinase.
Molecular pharmacology 2007;72(6):1593-8.
2007: Marcela Krecmerová; Antonín Holý; Radek Pohl; Milena Masojídková; Graciela Andrei; Lieve Naesens; Johan Neyts; Jan Balzarini; Erik De Clercq; Robert Snoeck
Ester prodrugs of cyclic 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-azacytosine: synthesis and antiviral activity.
Journal of medicinal chemistry 2007;50(23):5765-72.
2007: Romeo Romagnoli; Pier Giovanni Baraldi; Vincent Remusat; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Olga Cruz-Lopez; Delia Preti; Francesca Fruttarolo; Mojgan Aghazadeh Tabrizi; Jan Balzarini; Ernest Hamel
Synthesis and biological evaluation of 2-amino-3-(3', 4', 5'-trimethoxy-phenylsulfonyl)-5-aryl thiophenes as a new class of antitubulin agents.
Medicinal chemistry (Shāriqah (United Arab Emirates)) 2007;3(6):507-12.
2007: Ineke Van Daele; Hélène Munier-Lehmann; Matheus Froeyen; Jan Balzarini; Serge Van Calenbergh
Rational design of 5'-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growth.
Journal of medicinal chemistry 2007;50(22):5281-92.
2007: Subhas Somalingappa Karki; Sreekanth Thota; Satyanarayana Y Darj; Jan Balzarini; Erik De Clercq
Synthesis, anticancer, and cytotoxic activities of some mononuclear Ru(II) compounds.
Bioorganic & medicinal chemistry 2007;15(21):6632-41.
2007: Carlos García-Aparicio; Alberto Diez-Torrubia; Jan Balzarini; Anne-Marie Lambeir; Sonsoles Velázquez; María-José Camarasa
Efficient conversion of tetrapeptide-based TSAO prodrugs to the parent drug by dipeptidyl-peptidase IV (DPPIV/CD26).
Antiviral research 2007;76(2):130-9.
2007: Ibrahim I Ozturk; Sotiris K Hadjikakou; Nick Hadjiliadis; Nikolaos Kourkoumelis; Maciej Kubicki; Martin Baril; Ian S Butler; Jan Balzarini
Synthesis, structural characterization, and biological studies of new antimony(III) complexes with thiones. The influence of the solvent on the geometry of the complexes.
Inorganic chemistry 2007;46(21):8652-61.
2007: Dani Youssef; Christie E Nichols; T Stanley Cameron; Jan Balzarini; Erik De Clercq; Amitabh Jha
Design, synthesis, and cytostatic activity of novel cyclic curcumin analogues.
Bioorganic & medicinal chemistry letters 2007;17(20):5624-9.
2007: Francesca Ceccherini-Silberstein; Valentina Svicher; Tobias Sing; Anna Artese; Maria Mercedes Santoro; Federica Forbici; Ada Bertoli; Stefano Alcaro; Guido Palamara; Antonella d'Arminio Monforte; Jan Balzarini; Andrea Antinori; Thomas Lengauer; Carlo Federico Perno
Characterization and structural analysis of novel mutations in human immunodeficiency virus type 1 reverse transcriptase involved in the regulation of resistance to nonnucleoside inhibitors.
Journal of virology 2007;81(20):11507-19.
2007: Claire Bertaux; Dirk Daelemans; Laurent Meertens; Emmanuel G Cormier; John F Reinus; Willy J Peumans; Els J M Van Damme; Yasuhiro Igarashi; Toshikazu Oki; Dominique Schols; Tanya Dragic; Jan Balzarini
Entry of hepatitis C virus and human immunodeficiency virus is selectively inhibited by carbohydrate-binding agents but not by polyanions.
Virology 2007;366(1):40-50.
2007: Olesya A Troshina; pavel troshin; Alexander S Peregudov; Viacheslav I Kozlovskiy; Jan Balzarini; Rimma N Lyubovskaya
Chlorofullerene C60Cl6: a precursor for straightforward preparation of highly water-soluble polycarboxylic fullerene derivatives active against HIV.
Organic & biomolecular chemistry 2007;5(17):2783-91.
2007: Amitabh Jha; Chandrani Mukherjee; Ashok K Prasad; Virinder S Parmar; Erik De Clercq; Jan Balzarini; James P Stables; Elias K Manavathu; Anuraag Shrivastav; Rajendra K Sharma; Kurt H Nienaber; Gordon A Zello; Jonathan R Dimmock
E,E,E-1-(4-Arylamino-4-oxo-2-butenoyl)-3,5-bis(arylidene)-4-piperidones: a topographical study of some novel potent cytotoxins.
Bioorganic & medicinal chemistry 2007;15(17):5854-65.
2007: Els Keyaerts; Leen Vijgen; Christophe Pannecouque; Els J M Van Damme; Willy J Peumans; Herman Egberink; Jan Balzarini; Marc Van Ranst
Plant lectins are potent inhibitors of coronaviruses by interfering with two targets in the viral replication cycle.
Antiviral research 2007;75(3):179-87.
2007: Tatjana Gazivoda; Mario Sokcević; Marijeta Kralj; Lidija Suman; Kresimir Pavelić; Erik De Clercq; Graciela Andrei; Robert Snoeck; Jan Balzarini; Mladen Mintas; Silvana Raić-Malić
Synthesis and antiviral and cytostatic evaluations of the new C-5 substituted pyrimidine and furo[2,3-d]pyrimidine 4',5'-didehydro-L-ascorbic acid derivatives.
Journal of medicinal chemistry 2007;50(17):4105-12.
2007: Amitabh Jha; Chandrani Mukherjee; Alfred J Rolle; Erik De Clercq; Jan Balzarini; James P Stables
Cytostatic activity of novel 4'-aminochalcone-based imides.
Bioorganic & medicinal chemistry letters 2007;17(16):4545-50.
2007: Miguel Stevens; Jan Balzarini; Irene M Lagoja; Bernard Noppen; Katrien François; Arthur Van Aerschot; Piet Herdewijn; Erik De Clercq; Christophe Pannecouque
Inhibition of human immunodeficiency virus type 1 transcription by N-aminoimidazole derivatives.
Virology 2007;365(1):220-37.
2007: Morris J Robins; Ireneusz Nowak; Vivek K Rajwanshi; Karl Miranda; John F Cannon; Matt Peterson; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Synthesis and antiviral evaluation of 6-(alkyl-heteroaryl)furo[2,3-d]pyrimidin-2(3H)-one nucleosides and analogues with ethynyl, ethenyl, and ethyl spacers at C6 of the furopyrimidine core.
Journal of medicinal chemistry 2007;50(16):3897-905.
2007: Jan Balzarini
Targeting the glycans of glycoproteins: a novel paradigm for antiviral therapy.
Nature reviews. Microbiology 2007;5(8):583-97.
2007: Youcef Mehellou; Christopher McGuigan; Andrea Brancale; Jan Balzarini
Design, synthesis, and anti-HIV activity of 2',3'-didehydro-2',3'-dideoxyuridine (d4U), 2',3'-dideoxyuridine (ddU) phosphoramidate 'ProTide' derivatives.
Bioorganic & medicinal chemistry letters 2007;17(13):3666-9.
2007: Jan Balzarini; Barbara Orzeszko; Jan K Maurin; Andrzej Orzeszko
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
European journal of medicinal chemistry 2007;42(7):993-1003.
2007: Svjetlana Prekupec; Damjan Makuc; Janez Plavec; Lidija Suman; Marijeta Kralj; Kresimir Pavelić; Jan Balzarini; Erik De Clercq; Mladen Mintas; Silvana Raić-Malić
Novel C-6 fluorinated acyclic side chain pyrimidine derivatives: synthesis, (1)H and (13)C NMR conformational studies, and antiviral and cytostatic evaluations.
Journal of medicinal chemistry 2007;50(13):3037-45.
2007: Satish K Chitneni; Christophe M Deroose; Humphrey Fonge; Rik Gijsbers; Natalia Dyubankova; Jan Balzarini; zeger debyser; Luc Mortelmans; Alfons Verbruggen; Guy Bormans
Synthesis and biological evaluation of an 123I-labeled bicyclic nucleoside analogue (BCNA) as potential SPECT tracer for VZV-tk reporter gene imaging.
Bioorganic & medicinal chemistry letters 2007;17(12):3458-62.
2007: Walter A Cristofoli; Leonard I Wiebe; Erik De Clercq; Graciela Andrei; Robert Snoeck; Jan Balzarini; Edward E Knaus
5-alkynyl analogs of arabinouridine and 2'-deoxyuridine: cytostatic activity against herpes simplex virus and varicella-zoster thymidine kinase gene-transfected cells.
Journal of medicinal chemistry 2007;50(12):2851-7.
2007: Xinying Zhang; Adel Amer; Xuesen Fan; Jan Balzarini; Johan Neyts; Erik De Clercq; Mark Prichard; Earl Kern; Paul F Torrence
Synthesis and antiviral activities of new acyclic and "double-headed" nucleoside analogues.
Bioorganic chemistry 2007;35(3):221-32.
2007: Yongting Luo; Xiaochao Xu; Jiwei Liu; Jian Li; Yisheng Sun; Zhen Liu; Jinzhi Liu; Els Van Damme; Jan Balzarini; Jinku Bao
A novel mannose-binding tuber lectin from Typhonium divaricatum (L.) Decne (family Araceae) with antiviral activity against HSV-II and anti-proliferative effect on human cancer cell lines.
Journal of biochemistry and molecular biology 2007;40(3):358-67.
2007: Jan Balzarini
The alpha(1,2)-mannosidase I inhibitor 1-deoxymannojirimycin potentiates the antiviral activity of carbohydrate-binding agents against wild-type and mutant HIV-1 strains containing glycan deletions in gp120.
FEBS letters 2007;581(10):2060-4.
2007: Romeo Romagnoli; Pier Giovanni Baraldi; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Delia Preti; Francesca Fruttarolo; Maria Giovanna Pavani; Mojgan Aghazadeh Tabrizi; Manlio Tolomeo; Stefania Grimaudo; Antonietta Di Cristina; Jan Balzarini; John A Hadfield; Andrea Brancale; Ernest Hamel
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
Journal of medicinal chemistry 2007;50(9):2273-7.
2007: Weiqiang Huang; Marvin J Miller; Erik De Clercq; Jan Balzarini
Syntheses and anti-HIV activities of (+/-)-norcarbovir and (+/-)-norabacavir.
Organic & biomolecular chemistry 2007;5(8):1164-6.
2007: Lei Ji; Fen-Er Chen; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or alpha-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
Journal of medicinal chemistry 2007;50(8):1778-86.
2007: Nunzia Ciliberti; Stefano Manfredini; Angela Angusti; Elisa Durini; Nicola Solaroli; Silvia Vertuani; Lisa Buzzoni; Maria Cruz Bonache; Efrat Ben-Shalom; Anna Karlsson; Ann Saada (Reisch); Jan Balzarini
Novel selective human mitochondrial kinase inhibitors: design, synthesis and enzymatic activity.
Bioorganic & medicinal chemistry 2007;15(8):3065-81.
2007: Dana Huskens; Kristel Van Laethem; Kurt Vermeire; Jan Balzarini; Dominique Schols
Resistance of HIV-1 to the broadly HIV-1-neutralizing, anti-carbohydrate antibody 2G12.
Virology 2007;360(2):294-304.
2007: Nicolas Gisch; Jan Balzarini; Chris Meier
Enzymatically activated cycloSal-d4T-monophosphates: The third generation of cycloSal-pronucleotides.
Journal of medicinal chemistry 2007;50(7):1658-67.
2007: Sofie Celen; Tjibbe de Groot; Jan Balzarini; Kathleen Vunckx; Christelle Terwinghe; Peter Vermaelen; Lizette Van Berckelaer; Hubert P Vanbilloen; Johan Nuyts; Luc Mortelmans; Alfons Verbruggen; Guy Bormans
Synthesis and evaluation of a (99m)Tc-MAMA-propyl-thymidine complex as a potential probe for in vivo visualization of tumor cell proliferation with SPECT.
Nuclear medicine and biology 2007;34(3):283-91.
2007: Maria Letizia Barreca; Angela Rao; Laura De Luca; Nunzio Iraci; Anna Maria Monforte; giovanni maga; Erik De Clercq; Christophe Pannecouque; Jan Balzarini; Alba Chimirri
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
Bioorganic & medicinal chemistry letters 2007;17(7):1956-60.
2007: Miguel Stevens; Michela Pollicita; Christophe Pannecouque; Erik Verbeken; Oriana Tabarrini; Violetta Cecchetti; Stefano Aquaro; Carlo Federico Perno; Arnaldo Fravolini; Erik De Clercq; Dominique Schols; Jan Balzarini
Novel in vivo model for the study of human immunodeficiency virus type 1 transcription inhibitors: evaluation of new 6-desfluoroquinolone derivatives.
Antimicrobial agents and chemotherapy 2007;51(4):1407-13.
2007: Christian Ducho; Ulf Görbig; Sönke Jessel; Nicolas Gisch; Jan Balzarini; Chris Meier
Bis-cycloSal-d4T-monophosphates: drugs that deliver two molecules of bioactive nucleotides.
Journal of medicinal chemistry 2007;50(6):1335-46.
2007: Marcela Krecmerová; Antonín Holý; Alois Pískala; Milena Masojídková; Graciela Andrei; Lieve Naesens; Johan Neyts; Jan Balzarini; Erik De Clercq; Robert Snoeck
Antiviral activity of triazine analogues of 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]cytosine (cidofovir) and related compounds.
Journal of medicinal chemistry 2007;50(5):1069-77.
2007: Satish K Chitneni; Christophe M Deroose; Jan Balzarini; Rik Gijsbers; Sofie Celen; Tjibbe de Groot; zeger debyser; Luc Mortelmans; Alfons Verbruggen; Guy Bormans
Synthesis and preliminary evaluation of 18F- or 11C-labeled bicyclic nucleoside analogues as potential probes for imaging varicella-zoster virus thymidine kinase gene expression using positron emission tomography.
Journal of medicinal chemistry 2007;50(5):1041-9.
2007: Jan Balzarini; Lut Van Damme
Microbicide drug candidates to prevent HIV infection.
Lancet 2007;369(9563):787-97.
2007: Hari N Pati; Umashankar Das; Erik De Clercq; Jan Balzarini; Jonathan R Dimmock
Molecular modifications of 2-arylidene-1-indanones leading to increased cytotoxic potencies.
Journal of enzyme inhibition and medicinal chemistry 2007;22(1):37-42.
2007: Lei Ji; Fen-Er Chen; Bin Xie; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Synthesis and anti-HIV activity evaluation of 1-[(alkenyl or alkynyl or alkyloxy)methyl]-5-alkyl-6-(1-naphthoyl)-2,4-pyrimidinediones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
European journal of medicinal chemistry 2007;42(2):198-204.
2007: Tatjana Gazivoda; Silvana Raić-Malić; Marko Marjanović; Marijeta Kralj; Kresimir Pavelić; Jan Balzarini; Erik De Clercq; Mladen Mintas
The novel C-5 aryl, alkenyl, and alkynyl substituted uracil derivatives of L-ascorbic acid: synthesis, cytostatic, and antiviral activity evaluations.
Bioorganic & medicinal chemistry 2007;15(2):749-58.
2007: Nicolas Gisch; Jan Balzarini; Chris Meier
5-diacetoxymethyl-cycloSal-d4TMP - A prototype of enzymatically activated cycloSal-pronucleotides.
Nucleosides, nucleotides & nucleic acids 2007;26(6-7):861-4.
2007: Ulf Görbig; Jan Balzarini; Chris Meier
New cycloAmb-nucleoside phosphonate prodrugs.
Nucleosides, nucleotides & nucleic acids 2007;26(6-7):831-4.
2007: Sonia De Castro; Graziela Andrei; Robert Snoeck; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
Novel non-nucleoside human cytomegalovirus inhibitors based upon TSAO nucleoside derivatives: structure-activity relationships.
Nucleosides, nucleotides & nucleic acids 2007;26(6-7):625-8.
2007: Tokumi Maruyama; Yosuke Demizu; Shigetada Kozai; Myriam Witvrouw; Christophe Pannecouque; Jan Balzarini; Robert Snoecks; Graciela Andrei; Erik De Clercq
Antiviral activity of 3-(3,5-dimethylbenzyl)uracil derivatives against HIV-1 and HCMV.
Nucleosides, nucleotides & nucleic acids 2007;26(10-12):1553-8.
2007: Vincent Roy; Hiroki Kumamoto; Sabine Berteina-Raboin; Steven P Nolan; Dimitri Topalis; Dominique Deville-Bonne; Jan Balzarini; Johan Neyts; Gracelia Andrei; Robert Snoeck; Luigi A Agrofoglio
Cross-metathesis mediated synthesis of new acyclic nucleoside phosphonates.
Nucleosides, nucleotides & nucleic acids 2007;26(10-12):1399-402.
2007: Julie Broggi; Nicolas Joubert; Vincent Aucagne; Sabine Berteina-Raboin; S Diez-Gonzalez; Steve Nolan; Dimitri Topalis; Dominique Deville-Bonne; Jan Balzarini; Johan Neyts; Graciela Andrei; Robert Snoeck; Luigi A Agrofoglio
Alkyne-azide click chemistry mediated carbanucleosides synthesis.
Nucleosides, nucleotides & nucleic acids 2007;26(10-12):1391-4.
2007: Dalibor Vukadinović-Tenter; Jan Balzarini; Chris Meier
New developments of the "lock-in" modified cycloSal-d4TMPs.
Nucleosides, nucleotides & nucleic acids 2007;26(10-12):1325-8.
2007: HELA SAIDI; Nadine Nasreddine; Mohammad-Ali Jenabian; Maxime Lecerf; Dominique Schols; Corinne Krief; Jan Balzarini; Laurent Bélec
Differential in vitro inhibitory activity against HIV-1 of alpha-(1-3)- and alpha-(1-6)-D-mannose specific plant lectins: implication for microbicide development.
Journal of translational medicine 2007;5():28.
2007: Jiwei Liu; Xiaochao Xu; Jinzhi Liu; Jan Balzarini; Yongtin Luo; Yang Kong; Jian Li; Fang Chen; Els Van Damme; Jinku Bao
A novel tetrameric lectin from Lycoris aurea with four mannose binding sites per monomer.
Acta biochimica Polonica 2007;54(1):159-66.
2007: Jan Balzarini
Carbohydrate-binding agents: a potential future cornerstone for the chemotherapy of enveloped viruses?
Antiviral chemistry & chemotherapy 2007;18(1):1-11.
2007: Jan Balzarini; Dominique Schols; Kristel Van Laethem; Erik De Clercq; Dana Hocková; Milina Masojidkova; Antonín Holý
Pronounced in vitro and in vivo antiretroviral activity of 5-substituted 2,4-diamino-6-[2-(phosphonomethoxy)ethoxy] pyrimidines.
The Journal of antimicrobial chemotherapy 2007;59(1):80-6.
2007: Jan Balzarini; Yven Van Herrewege; Kurt Vermeire; Guido Vanham; Dominique Schols
Carbohydrate-binding agents efficiently prevent dendritic cell-specific intercellular adhesion molecule-3-grabbing nonintegrin (DC-SIGN)-directed HIV-1 transmission to T lymphocytes.
Molecular pharmacology 2007;71(1):3-11.
2007: Jan Balzarini; Kristel Van Laethem; Dirk Daelemans; Sigrid Hatse; Antonella Bugatti; MARCO RUSNATI; Yasuhiro Igarashi; Toshikazu Oki; Dominique Schols
Pradimicin A, a carbohydrate-binding nonpeptidic lead compound for treatment of infections with viruses with highly glycosylated envelopes, such as human immunodeficiency virus.
Journal of virology 2007;81(1):362-73.
2007: Umashankar Das; Jane Alcorn; Anuraag Shrivastav; Rajendra K Sharma; Erik De Clercq; Jan Balzarini; Jonathan R Dimmock
Design, synthesis and cytotoxic properties of novel 1-[4-(2-alkylaminoethoxy)phenylcarbonyl]-3,5-bis(arylidene)-4-piperidones and related compounds.
European journal of medicinal chemistry 2007;42(1):71-80.
2006: Karine Barral; Stéphane Priet; Joséphine Sire; Johan Neyts; Jan Balzarini; Bruno Canard; Karine Alvarez
Synthesis, in vitro antiviral evaluation, and stability studies of novel alpha-borano-nucleotide analogues of 9-[2-(phosphonomethoxy)ethyl]adenine and (R)-9-[2-(phosphonomethoxy)propyl]adenine.
Journal of medicinal chemistry 2006;49(26):7799-806.
2006: Ana-Isabel Hernandez; Olga Familiar; Ana Negri; Fátima Rodríguez-Barrios; Federico Gago; Anna Karlsson; María-José Camarasa; Jan Balzarini; María-Jesús Pérez-Pérez
N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.
Journal of medicinal chemistry 2006;49(26):7766-73.
2006: Vedran Kristafor; Silvana Raić-Malić; Mario Cetina; Marijeta Kralj; Lidija Suman; Kresimir Pavelić; Jan Balzarini; Erik De Clercq; Mladen Mintas
Synthesis, X-ray crystal structural study, antiviral and cytostatic evaluations of the novel unsaturated acyclic and epoxide nucleoside analogues.
Bioorganic & medicinal chemistry 2006;14(23):8126-38.
2006: Christopher McGuigan; Alshaimaa Hassan-Abdallah; Sheila Srinivasan; Yikang Wang; Adam Siddiqui; Susan M Daluge; Kristjan S Gudmundsson; Huiqiang Zhou; Ed W McLean; Jennifer P Peckham; Thimysta C Burnette; Harry Marr; Richard J Hazen; Lynn Condreay; Lance Johnson; Jan Balzarini
Application of phosphoramidate ProTide technology significantly improves antiviral potency of carbocyclic adenosine derivatives.
Journal of medicinal chemistry 2006;49(24):7215-26.
2006: Stefano Aquaro; Valentina Svicher; Dominique Schols; Michela Pollicita; Andrea Antinori; Jan Balzarini; Carlo Federico Perno
Mechanisms underlying activity of antiretroviral drugs in HIV-1-infected macrophages: new therapeutic strategies.
Journal of leukocyte biology 2006;80(5):1103-10.
2006: Romeo Romagnoli; Pier Giovanni Baraldi; Vincent Remusat; Maria Dora Carrion; LUISA-CARLOTA LÓPEZ-CARA; Delia Preti; Francesca Fruttarolo; Maria Giovanna Pavani; Mojgan Aghazadeh Tabrizi; Manlio Tolomeo; Stefania Grimaudo; Jan Balzarini; Mary Ann Jordan; Ernest Hamel
Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors.
Journal of medicinal chemistry 2006;49(21):6425-8.
2006: Kamel El Omari; Annelies Bronckaers; Sandra Liekens; María-Jesús Pérez-Pérez; Jan Balzarini; David K Stammers
Structural basis for non-competitive product inhibition in human thymidine phosphorylase: implications for drug design.
The Biochemical journal 2006;399(2):199-204.
2006: Jan Balzarini; Els Keyaerts; Leen Vijgen; Herman Egberink; Erik De Clercq; Marc Van Ranst; Svetlana S Printsevskaya; Evgenia N Olsufyeva; Svetlana E Solovieva; Maria N Preobrazhenskaya
Inhibition of feline (FIPV) and human (SARS) coronavirus by semisynthetic derivatives of glycopeptide antibiotics.
Antiviral research 2006;72(1):20-33.
2006: Sigrid Hatse; Jan Balzarini; Sandra Liekens
Stromal cell-derived factor 1 (CXCL12) binds to endothelial cells and signals through a receptor different from CXCR4.
Biochemical and biophysical research communications 2006;348(1):192-9.
2006: Elena Casanova; Ana-Isabel Hernandez; Eva-María Priego; Sandra Liekens; María-José Camarasa; Jan Balzarini; María-Jesús Pérez-Pérez
5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.
Journal of medicinal chemistry 2006;49(18):5562-70.
2006: Jan Balzarini
Large-molecular-weight carbohydrate-binding agents as HIV entry inhibitors targeting glycoprotein gp120.
Current opinion in HIV and AIDS 2006;1(5):355-60.
2006: Lei Ji; Fen-Er Chen; Xiao-Qing Feng; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Non-nucleoside HIV-1 reverse transcriptase inhibitors, Part 7. Synthesis, antiviral activity, and 3D-QSAR investigations of novel 6-(1-naphthoyl) HEPT analogues.
Chemical & pharmaceutical bulletin 2006;54(9):1248-53.
2006: Jan Balzarini; Kristel Van Laethem; Willy J Peumans; Els J M Van Damme; Anders Bolmstedt; Federico Gago; Dominique Schols
Mutational pathways, resistance profile, and side effects of cyanovirin relative to human immunodeficiency virus type 1 strains with N-glycan deletions in their gp120 envelopes.
Journal of virology 2006;80(17):8411-21.
2006: Miguel Stevens; Erik De Clercq; Jan Balzarini
The regulation of HIV-1 transcription: molecular targets for chemotherapeutic intervention.
Medicinal research reviews 2006;26(5):595-625.
2006: Carlo Federico Perno; Valentina Svicher; Dominique Schols; Michela Pollicita; Jan Balzarini; Stefano Aquaro
Therapeutic strategies towards HIV-1 infection in macrophages.
Antiviral research 2006;71(2-3):293-300.
2006: Chris Meier; Jan Balzarini
Application of the cycloSal-prodrug approach for improving the biological potential of phosphorylated biomolecules.
Antiviral research 2006;71(2-3):282-92.
2006: Christopher McGuigan; Jan Balzarini
Aryl furano pyrimidines: the most potent and selective anti-VZV agents reported to date.
Antiviral research 2006;71(2-3):149-53.
2006: Jan Balzarini
Inhibition of HIV entry by carbohydrate-binding proteins.
Antiviral research 2006;71(2-3):237-47.
2006: Carlos García-Aparicio; María-Cruz Bonache; Ingrid De Meester; Ana San-Félix; Jan Balzarini; María-José Camarasa; Sonsoles Velazquez
Design and discovery of a novel dipeptidyl-peptidase IV (CD26)-based prodrug approach.
Journal of medicinal chemistry 2006;49(17):5339-51.
2006: Nicolas Sluis-Cremer; Noureddine Hamamouch; Ana San-Félix; Sonsoles Velazquez; Jan Balzarini; María-José Camarasa
Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization.
Journal of medicinal chemistry 2006;49(16):4834-41.
2006: Sandra Liekens; Annelies Bronckaers; Ana-Isabel Hernández; Eva-María Priego; Elena Casanova; María-José Camarasa; María-Jesús Pérez-Pérez; Jan Balzarini
5'-O-tritylated nucleoside derivatives: inhibition of thymidine phosphorylase and angiogenesis.
Molecular pharmacology 2006;70(2):501-9.
2006: Sonia De Castro; Carlos García-Aparicio; Kristel Van Laethem; Federico Gago; Esther Lobatón; Erik De Clercq; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
Discovery of TSAO derivatives with an unusual HIV-1 activity/resistance profile.
Antiviral research 2006;71(1):15-23.
2006: Jan Balzarini; Sandra Liekens; Nicola Solaroli; Kamel El Omari; David K Stammers; Anna Karlsson
Engineering of a single conserved amino acid residue of herpes simplex virus type 1 thymidine kinase allows a predominant shift from pyrimidine to purine nucleoside phosphorylation.
The Journal of biological chemistry 2006;281(28):19273-9.
2006: Kamel El Omari; Sandra Liekens; Louise Bird; Jan Balzarini; David K Stammers
Mutations distal to the substrate site can affect varicella zoster virus thymidine kinase activity: implications for drug design.
Molecular pharmacology 2006;69(6):1891-6.
2006: Elisa Franzolin; Chiara Rampazzo; María-Jesús Pérez-Pérez; Ana-Isabel Hernández; Jan Balzarini; Vera Bianchi
Bromovinyl-deoxyuridine: A selective substrate for mitochondrial thymidine kinase in cell extracts.
Biochemical and biophysical research communications 2006;344(1):30-6.
2006: Tomasz Ostrowski; Bozenna Golankiewicz; Erik De Clercq; Jan Balzarini
Synthesis and biological activity of tricyclic analogues of 9-[[cis-1',2'-bis(hydroxymethyl)cycloprop-1'-yl]methyl]guanine.
Bioorganic & medicinal chemistry 2006;14(10):3535-42.
2006: Umashankar Das; Halise Inci Gul; Jane Alcorn; Anuraag Shrivastav; Theresa George; Rajendra K Sharma; Kurt H Nienaber; Erik De Clercq; Jan Balzarini; Masami Kawase; Noriyuki Kan; Toru Tanaka; Satoru Tani; Karl A Werbovetz; Adam J Yakovich; Elias K Manavathu; James P Stables; Jonathan R Dimmock
Cytotoxic 5-aryl-1-(4-nitrophenyl)-3-oxo-1,4-pentadienes mounted on alicyclic scaffolds.
European journal of medicinal chemistry 2006;41(5):577-85.
2006: Miguel Stevens; Christophe Pannecouque; Erik De Clercq; Jan Balzarini
Pyridine N-oxide derivatives inhibit viral transactivation by interfering with NF-kappaB binding.
Biochemical pharmacology 2006;71(8):1122-35.
2006: Tokumi Maruyama; Shigetada Kozai; Yosuke Demizu; Myriam Witvrouw; Christophe Pannecouque; Jan Balzarini; Robert Snoecks; Graciela Andrei; Erik De Clercq
Synthesis and anti-HIV-1 and anti-HCMV activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil derivatives.
Chemical & pharmaceutical bulletin 2006;54(3):325-33.
2006: Jan Balzarini; Els Keyaerts; Leen Vijgen; Frank Vandermeer; Miguel Stevens; Erik De Clercq; Herman Egberink; Marc Van Ranst
Pyridine N-oxide derivatives are inhibitory to the human SARS and feline infectious peritonitis coronavirus in cell culture.
The Journal of antimicrobial chemotherapy 2006;57(3):472-81.
2006: Jie An; Jin-Zhi Liu; Chuan-Fang Wu; Jian Li; Lei Dai; Els Van Damme; Jan Balzarini; Erik De Clercq; Fang Chen; Jin-Ku Bao
Anti-HIV I/II activity and molecular cloning of a novel mannose/sialic acid-binding lectin from rhizome of Polygonatum cyrtonema Hua.
Acta biochimica et biophysica Sinica 2006;38(2):70-8.
2006: Morris J Robins; Karl Miranda; Vivek K Rajwanshi; Matt Peterson; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Synthesis and biological evaluation of 6-(alkyn-1-yl)furo[2,3-d]pyrimidin-2(3H)-one base and nucleoside derivatives.
Journal of medicinal chemistry 2006;49(1):391-8.
2006: Karine Barral; Jan Balzarini; Johan Neyts; Erik De Clercq; Robert C Hider; Michel Camplo
Synthesis and antiviral evaluation of cyclic and acyclic 2-methyl-3-hydroxy-4-pyridinone nucleoside derivatives.
Journal of medicinal chemistry 2006;49(1):43-50.
2006: Zrinka Rajic; Branka Zorc; Silvana Raic-Malic; Katja Ester; Marijeta Kralj; Kresimir Pavelic; Jan Balzarini; Erik De Clercq; Mladen Mintas
Hydantoin derivatives of L- and D-amino acids: synthesis and evaluation of their antiviral and antitumoral activity.
Molecules (Basel, Switzerland) 2006;11(11):837-48.
2006: Sandra Liekens; Jan Balzarini; Ana-Isabel Hernández; Erik De Clercq; Eva-María Priego; María-José Camarasa; María-Jesús Pérez-Pérez
Thymidine phosphorylase is noncompetitively inhibited by 5'-O-trityl-inosine (KIN59) and related compounds.
Nucleosides, nucleotides & nucleic acids 2006;25(9-11):975-80.
2006: Kamel El Omari; Nicola Solaroli; Anna Karlsson; Jan Balzarini; David K Stammers
Structure of vaccinia virus thymidine kinase in complex with dTTP: insights for drug design.
BMC structural biology 2006;6():22.
2006: Paul Proost; Sofie Struyf; Tamara Loos; Mieke Gouwy; Evemie Schutyser; René Conings; Isabelle Ronsse; Marc Parmentier; Bernard Grillet; Ghislain Opdenakker; Jan Balzarini; Jo Van Damme
Coexpression and interaction of CXCL10 and CD26 in mesenchymal cells by synergising inflammatory cytokines: CXCL8 and CXCL10 are discriminative markers for autoimmune arthropathies.
Arthritis research & therapy 2006;8(4):R107.
2006: Jan Balzarini; Sofie Celen; Anna Karlsson; Tjibbe de Groot; Alfons Verbruggen; Guy Bormans
The effect of a methyl or 2-fluoroethyl substituent at the N-3 position of thymidine, 3'-fluoro-3'-deoxythymidine and 1-beta-D-arabinosylthymine on their antiviral and cytostatic activity in cell culture.
Antiviral chemistry & chemotherapy 2006;17(1):17-23.
2005: Chris Meier; Ulf Görbig; Christian Müller; Jan Balzarini
cycloSal-PMEA and cycloAmb-PMEA: potentially new phosphonate prodrugs based on the cycloSal-pronucleotide approach.
Journal of medicinal chemistry 2005;48(25):8079-86.
2005: Jan Balzarini; Kristel Van Laethem; Sigrid Hatse; Matheus Froeyen; Willy J Peumans; Els J M Van Damme; Dominique Schols
Carbohydrate-binding agents cause deletions of highly conserved glycosylation sites in HIV GP120: a new therapeutic concept to hit the achilles heel of HIV.
The Journal of biological chemistry 2005;280(49):41005-14.
2005: María-Jesús Pérez-Pérez; Eva-María Priego; Ana-Isabel Hernández; María-José Camarasa; Jan Balzarini; Sandra Liekens
Thymidine phosphorylase inhibitors: recent developments and potential therapeutic applications.
Mini reviews in medicinal chemistry 2005;5(12):1113-23.
2005: Dimitri Topalis; Bruno Collinet; Cécile Gasse; Laurence Dugué; Jan Balzarini; Sylvie Pochet; Dominique Deville-Bonne
Substrate specificity of vaccinia virus thymidylate kinase.
The FEBS journal 2005;272(24):6254-65.
2005: Jan Balzarini
Targeting the glycans of gp120: a novel approach aimed at the Achilles heel of HIV.
The Lancet infectious diseases 2005;5(11):726-31.
2005: Stuart G Turville; Kurt Vermeire; Jan Balzarini; Dominique Schols
Sugar-binding proteins potently inhibit dendritic cell human immunodeficiency virus type 1 (HIV-1) infection and dendritic-cell-directed HIV-1 transfer.
Journal of virology 2005;79(21):13519-27.
2005: Miguel Stevens; Jan Balzarini; Oriana Tabarrini; Graciela Andrei; Robert Snoeck; Violetta Cecchetti; Arnaldo Fravolini; Erik De Clercq; Christophe Pannecouque
Cell-dependent interference of a series of new 6-aminoquinolone derivatives with viral (HIV/CMV) transactivation.
The Journal of antimicrobial chemotherapy 2005;56(5):847-55.
2005: María-Cruz Bonache; Cristina Chamorro; Sonsoles Velázquez; Erik De Clercq; Jan Balzarini; Fátima Rodríguez Barrios; Federico Gago; María-José Camarasa; Ana San-Félix
Improving the antiviral efficacy and selectivity of HIV-1 reverse transcriptase inhibitor TSAO-T by the introduction of functional groups at the N-3 position.
Journal of medicinal chemistry 2005;48(21):6653-60.
2005: Guang-Fu Sun; Yun-Yan Kuang; Fen-Er Chen; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Non-nucleoside HIV reverse transcriptase inhibitors, Part 6[1]: synthesis and anti-HIV activity of novel 2-[(arylcarbonylmethyl)thio]-6-arylthio DABO analogues.
Archiv der Pharmazie 2005;338(10):457-61.
2005: LUISA-CARLOTA LÓPEZ-CARA; Pier Giovanni Baraldi; M Katherine Jung; Maria Antonietta Iaconinoto; Maria Dora Carrion; Vincent Remusat; Delia Preti; Mojgan Aghazadeh Tabrizi; Fruttarolo Francesca; Erik De Clercq; Jan Balzarini; Ernest Hamel
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
Bioorganic & medicinal chemistry letters 2005;15(18):4048-52.
2005: Joeri Auwerx; Fátima Rodríguez-Barrios; Francesca Ceccherini-Silberstein; Ana San-Félix; Sonsoles Velázquez; Erik De Clercq; María-José Camarasa; Carlo Federico Perno; Federico Gago; Jan Balzarini
The role of Thr139 in the human immunodeficiency virus type 1 reverse transcriptase sensitivity to (+)-calanolide A.
Molecular pharmacology 2005;68(3):652-9.
2005: Giovanna M Luoni; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic nucleoside inhibitors of Varicella-Zoster virus: the effect of branching in the p-alkylphenyl side chain.
Bioorganic & medicinal chemistry letters 2005;15(16):3791-6.
2005: Guang-Fu Sun; Xu-Xiang Chen; Fen-Er Chen; Yue-Ping Wang; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Nonnucleoside HIV-1 reverse-transcriptase inhibitors, part 5. Synthesis and anti-HIV-1 activity of novel 6-naphthylthio HEPT analogues.
Chemical & pharmaceutical bulletin 2005;53(8):886-92.
2005: Francesca Ceccherini-Silberstein; Federico Gago; Maria Santoro; Caterina Gori; Valentina Svicher; Fátima Rodríguez-Barrios; Roberta D'Arrigo; Massimo Ciccozzi; Ada Bertoli; Antonella d'Arminio Monforte; Jan Balzarini; Andrea Antinori; Carlo Federico Perno
High sequence conservation of human immunodeficiency virus type 1 reverse transcriptase under drug pressure despite the continuous appearance of mutations.
Journal of virology 2005;79(16):10718-29.
2005: Ada Bertoli; Maribel Franco; Jan Balzarini; Magnus Johansson; Anna Karlsson
Altered deoxyribonucleotide pools in T-lymphoblastoid cells expressing the multisubstrate nucleoside kinase of Drosophila melanogaster.
The FEBS journal 2005;272(15):3918-28.
2005: Silvia Marchesan; Tatiana Da Ros; Giampiero Spalluto; Jan Balzarini; Maurizio Prato
Anti-HIV properties of cationic fullerene derivatives.
Bioorganic & medicinal chemistry letters 2005;15(15):3615-8.
2005: Michael Breuer; Arnold De Loof; Jan Balzarini; Roger Huybrechts
Insecticidal activity of the pyrimidine nucleoside analogue (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU).
Pest management science 2005;61(8):737-41.
2005: Zlatko Janeba; Jan Balzarini; Graciela Andrei; Robert Snoeck; Erik De Clercq; Morris J Robins
Synthesis and biological evaluation of acyclic 3-[(2-hydroxyethoxy)methyl] analogues of antiviral furo- and pyrrolo[2,3-d]pyrimidine nucleosides.
Journal of medicinal chemistry 2005;48(14):4690-6.
2005: Jan Balzarini; Joeri Auwerx; Fátima Rodríguez-Barrios; Allel Chedad; Viktor Farkas; Francesca Ceccherini-Silberstein; Carlos García-Aparicio; Sonsoles Velázquez; Erik De Clercq; Carlo Federico Perno; María-José Camarasa; Federico Gago
The amino acid Asn136 in HIV-1 reverse transcriptase (RT) maintains efficient association of both RT subunits and enables the rational design of novel RT inhibitors.
Molecular pharmacology 2005;68(1):49-60.
2005: Albert Nguyen Van Nhien; Cyrille Tomassi; Christophe Len; José Marco-Contelles; Jan Balzarini; Christophe Pannecouque; Erik De Clercq; Denis Postel
First synthesis and evaluation of the inhibitory effects of aza analogues of TSAO on HIV-1 replication.
Journal of medicinal chemistry 2005;48(13):4276-84.
2005: Svetlana S Printsevskaya; Svetlana E Solovieva; Evgenia N Olsufyeva; Elena P Mirchink; Elena B Isakova; Erik De Clercq; Jan Balzarini; Maria N Preobrazhenskaya
Structure-activity relationship studies of a series of antiviral and antibacterial aglycon derivatives of the glycopeptide antibiotics vancomycin, eremomycin, and dechloroeremomycin.
Journal of medicinal chemistry 2005;48(11):3885-90.
2005: Stefano Aquaro; Valentina Svicher; Francesca Ceccherini-Silberstein; Alessandra Cenci; Fabbio Marcuccilli; Sara Giannella; Luisa Marcon; Raffaele Caliò; Jan Balzarini; Carlo Federico Perno
Limited development and progression of resistance of HIV-1 to the nucleoside analogue reverse transcriptase inhibitor lamivudine in human primary macrophages.
The Journal of antimicrobial chemotherapy 2005;55(6):872-8.
2005: Fátima Rodríguez-Barrios; Jan Balzarini; Federico Gago
The molecular basis of resilience to the effect of the Lys103Asn mutation in non-nucleoside HIV-1 reverse transcriptase inhibitors studied by targeted molecular dynamics simulations.
Journal of the American Chemical Society 2005;127(20):7570-8.
2005: Christopher McGuigan; Sarah A Harris; Susan M Daluge; Kristjan S Gudmundsson; Ed W McLean; Thimysta C Burnette; Harry Marr; Richard J Hazen; Lynn Condreay; Lance Johnson; Erik De Clercq; Jan Balzarini
Application of phosphoramidate pronucleotide technology to abacavir leads to a significant enhancement of antiviral potency.
Journal of medicinal chemistry 2005;48(10):3504-15.
2005: Maria Letizia Barreca; Angela Rao; Laura De Luca; Maria Zappalà; Anna Maria Monforte; giovanni maga; Christophe Pannecouque; Jan Balzarini; Erik De Clercq; Alba Chimirri; Pietro Monforte
Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT.
Journal of medicinal chemistry 2005;48(9):3433-7.
2005: Graciela Andrei; Jan Balzarini; Pierre Fiten; Erik De Clercq; Ghislain Opdenakker; Robert Snoeck
Characterization of herpes simplex virus type 1 thymidine kinase mutants selected under a single round of high-dose brivudin.
Journal of virology 2005;79(9):5863-9.
2005: Jan Balzarini; Kristel Van Laethem; Sigrid Hatse; Matheus Froeyen; Els J M Van Damme; Anders Bolmstedt; Willy J Peumans; Erik De Clercq; Dominique Schols
Marked depletion of glycosylation sites in HIV-1 gp120 under selection pressure by the mannose-specific plant lectins of Hippeastrum hybrid and Galanthus nivalis.
Molecular pharmacology 2005;67(5):1556-65.
2005: Joeri Auwerx; Joke Van Nieuwenhove; Fátima Rodríguez-Barrios; Sonia De Castro; Sonsoles Velázquez; Francesca Ceccherini-Silberstein; Erik De Clercq; María-José Camarasa; Carlo Federico Perno; Federico Gago; Jan Balzarini
The N137 and P140 amino acids in the p51 and the P95 amino acid in the p66 subunit of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase are instrumental to maintain catalytic activity and to design new classes of anti-HIV-1 drugs.
FEBS letters 2005;579(11):2294-300.
2005: Guillermo Gerona-Navarro; M Jesús Pérez de Vega; M Teresa García-López; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini; Rosario González-Muñiz
From 1-acyl-beta-lactam human cytomegalovirus protease inhibitors to 1-benzyloxycarbonylazetidines with improved antiviral activity. A straightforward approach to convert covalent to noncovalent inhibitors.
Journal of medicinal chemistry 2005;48(7):2612-21.
2005: Tomasz Ostrowski; Bozenna Golankiewicz; Erik De Clercq; Jan Balzarini
Fluorosubstitution and 7-alkylation as prospective modifications of biologically active 6-aryl derivatives of tricyclic acyclovir and ganciclovir analogues.
Bioorganic & medicinal chemistry 2005;13(6):2089-96.
2005: Graciela Andrei; Rebecca Sienaert; Christopher McGuigan; Erik De Clercq; Jan Balzarini; Robert Snoeck
Susceptibilities of several clinical varicella-zoster virus (VZV) isolates and drug-resistant VZV strains to bicyclic furano pyrimidine nucleosides.
Antimicrobial agents and chemotherapy 2005;49(3):1081-6.
2005: Lieve Naesens; L Lenaerts; Graciela Andrei; Robert Snoeck; Daniele Van Beers; Antonin Holy; Jan Balzarini; Erik De Clercq
Antiadenovirus activities of several classes of nucleoside and nucleotide analogues.
Antimicrobial agents and chemotherapy 2005;49(3):1010-6.
2005: Sonia De Castro; Esther Lobatón; María-Jesús Pérez-Pérez; Ana San-Félix; Alessandra Cordeiro; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
Novel [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2" -dioxide) derivatives with anti-HIV-1 and anti-human-cytomegalovirus activity.
Journal of medicinal chemistry 2005;48(4):1158-68.
2005: Jan Balzarini; Lut Van Damme
Intravaginal and intrarectal microbicides to prevent HIV infection.
CMAJ : Canadian Medical Association journal = journal de l'Association medicale canadienne 2005;172(4):461-4.
2005: Monika Barbarić; Stanko Ursić; Viktor Pilepić; Branka Zorc; Antonija Hergold-Brundić; Ante Nagl; Mira Grdisa; Kresimir Pavelić; Robert Snoeck; Graciela Andrei; Jan Balzarini; Erik De Clercq; Mladen Mintas
Synthesis, X-ray crystal structure study, and cytostatic and antiviral evaluation of the novel cycloalkyl-N-aryl-hydroxamic acids.
Journal of medicinal chemistry 2005;48(3):884-7.
2005: Pieter Leyssen; Jan Balzarini; Erik De Clercq; Johan Neyts
The predominant mechanism by which ribavirin exerts its antiviral activity in vitro against flaviviruses and paramyxoviruses is mediated by inhibition of IMP dehydrogenase.
Journal of virology 2005;79(3):1943-7.
2005: Jan Balzarini; Miguel Stevens; Erik De Clercq; Dominique Schols; Christophe Pannecouque
Pyridine N-oxide derivatives: unusual anti-HIV compounds with multiple mechanisms of antiviral action.
The Journal of antimicrobial chemotherapy 2005;55(2):135-8.
2005: Ninoslav Opacić; Monika Barbarić; Branka Zorc; Mario Cetina; Ante Nagl; Danijel Frković; Marijeta Kralj; Kresimir Pavelić; Jan Balzarini; Graciela Andrei; Robert Snoeck; Erik De Clercq; Silvana Raić-Malić; Mladen Mintas
The novel L- and D-amino acid derivatives of hydroxyurea and hydantoins: synthesis, X-ray crystal structure study, and cytostatic and antiviral activity evaluations.
Journal of medicinal chemistry 2005;48(2):475-82.
2005: Karine Barral; Jérôme Courcambeck; Gérard Pèpe; Jan Balzarini; Johan Neyts; Erik De Clercq; Michel Camplo
Synthesis and antiviral evaluation of cis-substituted cyclohexenyl and cyclohexanyl nucleosides.
Journal of medicinal chemistry 2005;48(2):450-6.
2005: Tatjana Gazivoda; Miha Plevnik; Janez Plavec; Sandra Kraljević; Marijeta Kralj; Kresimir Pavelić; Jan Balzarini; Erik De Clercq; Mladen Mintas; Silvana Raić-Malić
The novel pyrimidine and purine derivatives of l-ascorbic acid: synthesis, one- and two-dimensional 1H and 13C NMR study, cytostatic and antiviral evaluation.
Bioorganic & medicinal chemistry 2005;13(1):131-9.
2005: Longhu Zhou; Adel Amer; Michael Korn; Robert Burda; Jan Balzarini; Erik De Clercq; Earl R Kern; Paul F Torrence
Synthesis and antiviral activities of 1,2,3-triazole functionalized thymidines: 1,3-dipolar cycloaddition for efficient regioselective diversity generation.
Antiviral chemistry & chemotherapy 2005;16(6):375-83.
2005: María-Jesús Pérez-Pérez; Ana-Isabel Hernández; Eva-María Priego; Fátima Rodríguez-Barrios; Federico Gago; María-José Camarasa; Jan Balzarini
Mitochondrial thymidine kinase inhibitors.
Current topics in medicinal chemistry 2005;5(13):1205-19.
2005: D Vukadinović; N P H Böge; Jan Balzarini; Chris Meier
"Lock-in" modified cyclosal nucleotides--the second generation of cyclosal prodrugs.
Nucleosides, nucleotides & nucleic acids 2005;24(5-7):939-42.
2005: M R Kelleher; Christopher McGuigan; Olivier Bidet; Antonella Carangio; H Weldon; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
The journey towards elucidating the anti-HCMV activity of alkylated bicyclic furano pyrimidines.
Nucleosides, nucleotides & nucleic acids 2005;24(5-7):643-5.
2005: Tomasz Goslinski; Piotr Januszczyk; Grazyna Wenska; Bozenna Golankiewicz; Erik De Clercq; Jan Balzarini
Synthesis and fluorescent properties of the tricyclic analogues of acyclovir linked with nitrogen hetbrocyclic units.
Nucleosides, nucleotides & nucleic acids 2005;24(5-7):571-5.
2005: Christian Ducho; Sönke Jessel; Nicolas Gisch; Jan Balzarini; Chris Meier
Novel cyclosal nucleotides with reduced inhibitory potency toward human butyrylcholinesterase.
Nucleosides, nucleotides & nucleic acids 2005;24(5-7):519-22.
2005: Erik De Clercq; Graciela Andrei; Jan Balzarini; Pieter Leyssen; Lieve Naesens; Johan Neyts; Christophe Pannecouque; Robert Snoeck; Chunxiao Ying; Dana Hocková; Antonín Holý
Antiviral potential of a new generation of acyclic nucleoside phosphonates, the 6-[2-(phosphonomethoxy)alkoxy]-2,4-diaminopyrimidines.
Nucleosides, nucleotides & nucleic acids 2005;24(5-7):331-41.
2005: Svjetlana Prekupec; Damjan Makuc; Janez Plavec; Sandra Kraljević; Marijeta Kralj; Kresimir Pavelić; Graciela Andrei; Robert Snoeck; Jan Balzarini; Erik De Clercq; Silvana Raić-Malić; Mladen Mintas
Antiviral and cytostatic evaluation of the novel 6-acyclic chain substituted thymine derivatives.
Antiviral chemistry & chemotherapy 2005;16(5):327-38.
2005: Elin Andersson; Peter Horal; Alenka Jejcic; Stefan Höglund; Jan Balzarini; Anders Vahlne; Bo Svennerholm
Glycine-amide is an active metabolite of the antiretroviral tripeptide glycyl-prolyl-glycine-amide.
Antimicrobial agents and chemotherapy 2005;49(1):40-4.
2004: Barbara Orzeszko; Zygmunt Kazimierczuk; Jan Krzysztof Maurin; Agnieszka Ewa Laudy; Bohdan Jerzy Starościak; Juhani Vilpo; Leena Vilpo; Jan Balzarini; Andrzej Orzeszko
Novel adamantylated pyrimidines and their preliminary biological evaluations.
Farmaco (Società chimica italiana : 1989) 2004;59(12):929-37.
2004: Yanping He; Fener Chen; Xiongjie Yu; Yueping Wang; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Nonnucleoside HIV-1 reverse transcriptase inhibitors; part 3. Synthesis and antiviral activity of 5-alkyl-2-[(aryl and alkyloxyl-carbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones.
Bioorganic chemistry 2004;32(6):536-48.
2004: Giovanna M Luoni; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic nucleoside inhibitors of varicella-zoster virus modified on the sugar moiety: 3' and 5' derivatives.
Antiviral chemistry & chemotherapy 2004;15(6):333-41.
2004: Olivier Bidet; Christopher McGuigan; Robert Snoeck; Graciela Andrei; Erik De Clercq; Jan Balzarini
Non-nucleoside structures retain full anti-HCMV potency of the dideoxy furanopyrimidine family.
Antiviral chemistry & chemotherapy 2004;15(6):329-32.
2004: Hannah L Maslen; David Hughes; Mike Hursthouse; Erik De Clercq; Jan Balzarini; Claire Simons
6-azapyrimidine-2'-deoxy-4'-thionucleosides: antiviral agents against TK+ and TK- HSV and VZV strains.
Journal of medicinal chemistry 2004;47(22):5482-91.
2004: Jan Balzarini; Christophe Pannecouque; Lieve Naesens; Graciela Andrei; Robert Snoeck; Erik De Clercq; Dana Hocková; Antonín Holý
6-[2-phosphonomethoxy)alkoxy]-2,4-diaminopyrimidines: a new class of acyclic pyrimidine nucleoside phosphonates with antiviral activity.
Nucleosides, nucleotides & nucleic acids 2004;23(8-9):1321-7.
2004: Jan Balzarini; Sigrid Hatse; Kurt Vermeire; Katrien Princen; Stefano Aquaro; Carlo Federico Perno; Erik De Clercq; Herman Egberink; Guy Vanden Mooter; Willy J Peumans; Els J M Van Damme; Dominique Schols
Mannose-specific plant lectins from the Amaryllidaceae family qualify as efficient microbicides for prevention of human immunodeficiency virus infection.
Antimicrobial agents and chemotherapy 2004;48(10):3858-70.
2004: Jan Balzarini; Kristel Van Laethem; Sigrid Hatse; Kurt Vermeire; Erik De Clercq; Willy J Peumans; Els Van Damme; Anne-Mieke Vandamme; Anders Bölmstedt; Dominique Schols; Anders Böhlmstedt
Profile of resistance of human immunodeficiency virus to mannose-specific plant lectins.
Journal of virology 2004;78(19):10617-27.
2004: Eva-María Priego; Jan Balzarini; Anna Karlsson; María-José Camarasa; María-Jesús Pérez-Pérez
Synthesis and evaluation of thymine-derived carboxamides against mitochondrial thymidine kinase (TK-2) and related enzymes.
Bioorganic & medicinal chemistry 2004;12(19):5079-90.
2004: Jan Balzarini; Elin Andersson; Dominique Schols; Paul Proost; Jo Van Damme; Bo Svennerholm; Peter Horal; Anders Vahlne
Obligatory involvement of CD26/dipeptidyl peptidase IV in the activation of the antiretroviral tripeptide glycylprolylglycinamide (GPG-NH(2)).
The international journal of biochemistry & cell biology 2004;36(9):1848-59.
2004: Jan Balzarini; Stefano Aquaro; Alshaimaa Hassan-Abdallah; Susan M Daluge; Carlo Federico Perno; Christopher McGuigan
Improved antiviral activity of the aryloxymethoxyalaninyl phosphoramidate (APA) prodrug of abacavir (ABC) is due to the formation of markedly increased carbovir 5'-triphosphate metabolite levels.
FEBS letters 2004;573(1-3):38-44.
2004: A Rao; Jan Balzarini; A Carbone; Alba Chimirri; Erik De Clercq; Anna Maria Monforte; Pietro Monforte; Christophe Pannecouque; Maria Zappalà
2-(2,6-Dihalophenyl)-3-(pyrimidin-2-yl)-1,3-thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
Antiviral research 2004;63(2):79-84.
2004: Nurolaini Kifli; Erik De Clercq; Jan Balzarini; Claire Simons
Novel imidazo[1,2-c]pyrimidine base-modified nucleosides: synthesis and antiviral evaluation.
Bioorganic & medicinal chemistry 2004;12(15):4245-52.
2004: Sandra Liekens; Ana-Isabel Hernández; Dragana Vukasovic; Erik De Clercq; María-José Camarasa; María-Jesús Pérez-Pérez; Jan Balzarini
The nucleoside derivative 5'-O-trityl-inosine (KIN59) suppresses thymidine phosphorylase-triggered angiogenesis via a noncompetitive mechanism of action.
The Journal of biological chemistry 2004;279(28):29598-605.
2004: Joeri Auwerx; Miguel Stevens; An R Van Rompay; Louise Bird; Jingshan Ren; Erik De Clercq; Bo Oberg; David K Stammers; Anna Karlsson; Jan Balzarini
The phenylmethylthiazolylthiourea nonnucleoside reverse transcriptase (RT) inhibitor MSK-076 selects for a resistance mutation in the active site of human immunodeficiency virus type 2 RT.
Journal of virology 2004;78(14):7427-37.
2004: Yanping He; Fener Chen; Guangfu Sun; Yueping Wang; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors of S-DABO series.
Bioorganic & medicinal chemistry letters 2004;14(12):3173-6.
2004: Sonsoles Velázquez; Esther Lobatón; Erik De Clercq; Dianna L Koontz; John W Mellors; Jan Balzarini; María-José Camarasa
Hybrids of [TSAO-T]-[foscarnet]: The first conjugate of foscarnet with a non-nucleoside reverse transcriptase inhibitor through a labile covalent ester bond.
Journal of medicinal chemistry 2004;47(13):3418-26.
2004: Nurolaini Kifli; Thet Thet Htar; Erik De Clercq; Jan Balzarini; Claire Simons
Novel bicyclic sugar modified nucleosides: synthesis, conformational analysis and antiviral evaluation.
Bioorganic & medicinal chemistry 2004;12(12):3247-57.
2004: Dana Hocková; Antonín Holý; Milena Masojídková; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Synthesis and antiviral activity of 2,4-diamino-5-cyano-6-[2-(phosphonomethoxy)ethoxy]pyrimidine and related compounds.
Bioorganic & medicinal chemistry 2004;12(12):3197-202.
2004: Pier Giovanni Baraldi; Maria Del Carmen Nunez; Mojgan Aghazadeh Tabrizi; Erik De Clercq; Jan Balzarini; Jaime Bermejo; Francisco Estévez; LUISA-CARLOTA LÓPEZ-CARA
Design, synthesis, and biological evaluation of hybrid molecules containing alpha-methylene-gamma-butyrolactones and polypyrrole minor groove binders.
Journal of medicinal chemistry 2004;47(11):2877-86.
2004: Chris Meier; Christian Ducho; Ulf Görbig; Robert M Esnouf; Jan Balzarini
Interaction of cycloSal-pronucleotides with cholinesterases from different origins. A structure-activity relationship.
Journal of medicinal chemistry 2004;47(11):2839-52.
2004: Annette Angell; Christopher McGuigan; Luis Garcia Sevillano; Robert Snoeck; Graciela Andrei; Erik De Clercq; Jan Balzarini
Bicyclic anti-VZV nucleosides: thieno analogues bearing an alkylphenyl side chain have reduced antiviral activity.
Bioorganic & medicinal chemistry letters 2004;14(10):2397-9.
2004: Guillermo Gerona-Navarro; M Jesús Pérez de Vega; M Teresa García-López; Graciela Andrei; Robert Snoeck; Jan Balzarini; Erik De Clercq; Rosario González-Muñiz
Synthesis and anti-HCMV activity of 1-acyl-beta-lactams and 1-acylazetidines derived from phenylalanine.
Bioorganic & medicinal chemistry letters 2004;14(9):2253-6.
2004: Chris Meier; Manuel F H Ruppel; Dalibor Vukadinovic; Jan Balzarini
"Lock-in"-cycloSal-pronucleotides - a new generation of chemical Trojan Horses?
Mini reviews in medicinal chemistry 2004;4(4):383-94.
2004: Dominique Cahard; Christopher McGuigan; Jan Balzarini
Aryloxy phosphoramidate triesters as pro-tides.
Mini reviews in medicinal chemistry 2004;4(4):371-81.
2004: Agnes Rinaldo-Matthis; Chiara Rampazzo; Jan Balzarini; Peter Reichard; Vera Bianchi; Pär Nordlund
Crystal structures of the mitochondrial deoxyribonucleotidase in complex with two specific inhibitors.
Molecular pharmacology 2004;65(4):860-7.
2004: Piet Borst; Jan Balzarini; Nobuhito Ono; Glen Reid; H de Vries; peter wielinga; Jan Wijnholds; Noam Zelcer
The potential impact of drug transporters on nucleoside-analog-based antiviral chemotherapy.
Antiviral research 2004;62(1):1-7.
2004: Christopher McGuigan; Ranjith N Pathirana; Robert Snoeck; Graciela Andrei; Erik De Clercq; Jan Balzarini
Discovery of a new family of inhibitors of human cytomegalovirus (HCMV) based upon lipophilic alkyl furano pyrimidine dideoxy nucleosides: action via a novel non-nucleosidic mechanism.
Journal of medicinal chemistry 2004;47(7):1847-51.
2004: Rebecca Sienaert; Graciela Andrei; Robert Snoeck; Erik De Clercq; Christopher McGuigan; Jan Balzarini
Inactivity of the bicyclic pyrimidine nucleoside analogues against simian varicella virus (SVV) does not correlate with their substrate activity for SVV-encoded thymidine kinase.
Biochemical and biophysical research communications 2004;315(4):877-83.
2004: Silvana Raić-Malić; Linda Tomasković; Draginja Mrvos-Sermek; Biserka Prugovecki; Mario Cetina; Mira Grdisa; Kresimir Pavelić; Albrecht Mannschreck; Jan Balzarini; Erik De Clercq; Mladen Mintas
Spirobipyridopyrans, spirobinaphthopyrans, indolinospiropyridopyrans, indolinospironaphthopyrans and indolinospironaphtho-1,4-oxazines: synthesis, study of X-ray crystal structure, antitumoral and antiviral evaluation.
Bioorganic & medicinal chemistry 2004;12(5):1037-45.
2004: Jonathan R Dimmock; Mahmood Chamankhah; Umashankar Das; Gordon A Zello; J Wilson Quail; J Yang; Kurt H Nienaber; Rajendra K Sharma; Ponniah Selvakumar; Jan Balzarini; Erik De Clercq; James P Stables
Cytotoxic and topographical properties of 6-arylidene-2-dimethylaminomethylcyclohexanone hydrochlorides and related compounds.
Journal of enzyme inhibition and medicinal chemistry 2004;19(1):1-10.
2004: Thomas C Rosen; Erik De Clercq; Jan Balzarini; Günter Haufe
Synthesis and antiviral activity of monofluorinated cyclopropanoid nucleosides.
Organic & biomolecular chemistry 2004;2(2):229-37.
2004: Jesús Mendieta; Sonsoles Martín-Santamaría; Eva-María Priego; Jan Balzarini; María-José Camarasa; María-Jesús Pérez-Pérez; Federico Gago
Role of histidine-85 in the catalytic mechanism of thymidine phosphorylase as assessed by targeted molecular dynamics simulations and quantum mechanical calculations.
Biochemistry 2004;43(2):405-14.
2004: Tokumi Maruyama; Shigetada Kozai; Yosuke Demizu; Myriam Witvrouw; Christophe Pannecouque; Jan Balzarini; Robert Snoeck; Graciela Andrei; Erik De Clercq
Synthesis and antiviral activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil against HIV-1.
Nucleic acids symposium series (2004) 2004;(48):3-4.
2004: Jürgen Voss; Jörn Wirsching; Oliver Schulze; Gunadi Adiwidjaja; Anja Giesler; Jan Balzarini; Erik De Clercq
Thiosugars. XII. Synthesis of new 3'-O-substituted 2',5'-anhydro-2'-thio-alpha-D-pentofuranosyl nucleoside analogues.
Nucleosides, nucleotides & nucleic acids 2004;23(10):1609-23.
2004: Chryssostomos Chatgilialoglu; Carla Ferreri; Thanasis Gimisis; Marinella Roberti; Jan Balzarini; Erik De Clercq
Synthesis and biological evaluation of novel 1'-branched and spironucleoside analogues.
Nucleosides, nucleotides & nucleic acids 2004;23(10):1565-81.
2004: Carlo Federico Perno; Emanuela Balestra; Mauro Francesconi; D Abdelahad; Raffaele Caliò; Jan Balzarini; Stefano Aquaro
Antiviral profile of HIV inhibitors in macrophages: implications for therapy.
Current topics in medicinal chemistry 2004;4(9):1009-15.
2004: María-José Camarasa; Ana San-Félix; Sonsoles Velázquez; María-Jesús Pérez-Pérez; Federico Gago; Jan Balzarini
TSAO compounds: the comprehensive story of a unique family of HIV-1 specific inhibitors of reverse transcriptase.
Current topics in medicinal chemistry 2004;4(9):945-63.
2004: Jan Balzarini
Current status of the non-nucleoside reverse transcriptase inhibitors of human immunodeficiency virus type 1.
Current topics in medicinal chemistry 2004;4(9):921-44.
2004: Chris Meier; Manuel F H Ruppel; Dalibor Vukadinović; Jan Balzarini
Second generation of cycloSal-pronucleotides with esterase-cleavable sites: the "lock-in"-concept.
Nucleosides, nucleotides & nucleic acids 2004;23(1-2):89-115.
2004: Suzana Jaksa; Bogdan Kralj; Christophe Pannecouque; Jan Balzarini; Erik De Clercq; Joze Kobe
How a modification (8-aza-3-deaza-2'-deoxyguanosine) influences the quadruplex structure of Hotoda's 6-mer TGGGAG with 5'- and 3'-end modifications.
Nucleosides, nucleotides & nucleic acids 2004;23(1-2):77-88.
2004: Piyush Kumar; Kazue Ohkura; Jan Balzarini; Erik De Clercq; Koh-ichi Seki; Leonard I Wiebe
Synthesis and antiviral activity of novel fluorinated 2',3'-dideoxynucleosides.
Nucleosides, nucleotides & nucleic acids 2004;23(1-2):7-29.
2004: Christopher McGuigan; Antonella Carangio; Robert Snoeck; Graciela Andrei; Erik De Clercq; Jan Balzarini
Synthesis and antiviral evaluation of some 3'-fluoro bicyclic nucleoside analogues.
Nucleosides, nucleotides & nucleic acids 2004;23(1-2):1-5.
2004: Sarvesh C Vashishtha; Gordon A Zello; Kurt H Nienaber; Jan Balzarini; Erik De Clercq; James P Stables; Jonathan R Dimmock
Cytotoxic and anticonvulsant aryloxyaryl Mannich bases and related compounds.
European journal of medicinal chemistry 2004;39(1):27-35.
2004: Chris Meier; Astrid Meerbach; Jan Balzarini
Cyclosal-pronucleotides--development of first and second generation chemical trojan horses for antiviral chemotherapy.
Frontiers in bioscience : a journal and virtual library 2004;9():873-90.
2004: Angela Rao; Jan Balzarini; Anna Carbone; Alba Chimirri; Erik De Clercq; Anna Maria Monforte; Pietro Monforte; Christophe Pannecouque; Maria Zappalà
Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
Farmaco (Società chimica italiana : 1989) 2004;59(1):33-9.
2004: Joeri Auwerx; Robert M Esnouf; Erik De Clercq; Jan Balzarini
Susceptibility of feline immunodeficiency virus/human immunodeficiency virus type 1 reverse transcriptase chimeras to non-nucleoside RT inhibitors.
Molecular pharmacology 2004;65(1):244-51.
2004: Yven Van Herrewege; Jo Michiels; Jens Van Roey; Katrien Fransen; Luc Kestens; Jan Balzarini; Paul J Lewi; Guido Vanham; Paul Janssen
In vitro evaluation of nonnucleoside reverse transcriptase inhibitors UC-781 and TMC120-R147681 as human immunodeficiency virus microbicides.
Antimicrobial agents and chemotherapy 2004;48(1):337-9.
2003: Svjetlana Prekupec; Drazenka Svedruzić; Tatjana Gazivoda; Draginja Mrvos-Sermek; Ante Nagl; Mira Grdisa; Kresimir Pavelić; Jan Balzarini; Erik De Clercq; Gerd Folkers; Leonardo Scapozza; Mladen Mintas; Silvana Raić-Malić
Synthesis and biological evaluation of iodinated and fluorinated 9-(2-hydroxypropyl) and 9-(2-hydroxyethoxy)methyl purine nucleoside analogues.
Journal of medicinal chemistry 2003;46(26):5763-72.
2003: Christopher McGuigan; Andrea Brancale; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Novel bicyclic furanopyrimidines with dual anti-VZV and -HCMV activity.
Bioorganic & medicinal chemistry letters 2003;13(24):4511-3.
2003: Susanna Bosi; Tatiana Da Ros; Giampiero Spalluto; Jan Balzarini; Maurizio Prato
Synthesis and anti-HIV properties of new water-soluble bis-functionalized[60]fullerene derivatives.
Bioorganic & medicinal chemistry letters 2003;13(24):4437-40.
2003: Karine Barral; Robert C Hider; Jan Balzarini; Johan Neyts; Erik De Clercq; Michel Camplo
Synthesis and antiviral evaluation of 3-hydroxy-2-methylpyridin-4-one dideoxynucleoside derivatives.
Bioorganic & medicinal chemistry letters 2003;13(24):4371-4.
2003: Dana Hocková; Antonín Holý; Milena Masojídková; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
5-Substituted-2,4-diamino-6-[2-(phosphonomethoxy)ethoxy]pyrimidines-acyclic nucleoside phosphonate analogues with antiviral activity.
Journal of medicinal chemistry 2003;46(23):5064-73.
2003: Jörn Wirsching; Jürgen Voss; Anja Giesler; Jürgen Kopf; Gunadi Adiwidjaja; Jan Balzarini; Erik De Clercq
Thiosugars. X. Novel nucleoside analogues derived from 4-thio-L-lyxofuranose.
Nucleosides, nucleotides & nucleic acids 2003;22(10):1867-97.
2003: Miguel Stevens; Christophe Pannecouque; Erik De Clercq; Jan Balzarini
Novel human immunodeficiency virus (HIV) inhibitors that have a dual mode of anti-HIV action.
Antimicrobial agents and chemotherapy 2003;47(10):3109-16.
2003: Ana-Isabel Hernández; Jan Balzarini; Fátima Rodríguez-Barrios; Ana San-Félix; Anna Karlsson; Federico Gago; María-José Camarasa; María-Jesús Pérez-Pérez
Improving the selectivity of acyclic nucleoside analogues as inhibitors of human mitochondrial thymidine kinase: replacement of a triphenylmethoxy moiety with substituted amines and carboxamides.
Bioorganic & medicinal chemistry letters 2003;13(18):3027-30.
2003: Tokumi Maruyama; Shigetada Kozai; Tetsuo Yamasaki; Myriam Witvrouw; Christophe Pannecouque; Jan Balzarini; Robert Snoeck; Graciela Andrei; Erik De Clercq
Synthesis and antiviral activity of 1,3-disubstituted uracils against HIV-1 and HCMV.
Antiviral chemistry & chemotherapy 2003;14(5):271-9.
2003: María-Cruz Bonache; Cristina Chamorro; Esther Lobatón; Erik De Clercq; Jan Balzarini; Sonsoles Velázquez; María-José Camarasa; Ana San-Félix
Structure-activity relationship studies on a novel family of specific HIV-1 reverse transcriptase inhibitors.
Antiviral chemistry & chemotherapy 2003;14(5):249-62.
2003: José Manuel Blanco; Olga Caamaño; Franco Fernández; José Enrique Rodríguez-Borges; Jan Balzarini; Erik De Clercq
Carbocyclic analogues of nucleosides from bis-(Hydroxymethyl)-cyclopentane: synthesis, antiviral and cytostatic activities of adenosine, inosine and uridine analogues.
Chemical & pharmaceutical bulletin 2003;51(9):1060-3.
2003: Miguel Stevens; Christophe Pannecouque; Erik De Clercq; Jan Balzarini
Inhibition of human immunodeficiency virus by a new class of pyridine oxide derivatives.
Antimicrobial agents and chemotherapy 2003;47(9):2951-7.
2003: Jonathan R Dimmock; Amitabh Jha; Gordon A Zello; Rajendra K Sharma; Anuraag Shrivastav; Ponniah Selvakumar; Theresa M Allen; Cheryl L Santos; Jan Balzarini; Erik De Clercq; Elias K Manavathu; James P Stables
3,5-bis(phenylmethylene)-1-(N-arylmaleamoyl)-4-piperidones: a novel group of cytotoxic agents.
Journal of enzyme inhibition and medicinal chemistry 2003;18(4):325-32.
2003: Jonathan R Dimmock; Maniyan Padmanilayam; Umashankar Das; Gordon A Zello; Rajendra K Sharma; Anuraag Shrivastav; Ponniah Selvakumar; Mohammed Khysar Pasha; Kurt H Nienaber; Jeremy S Lee; Theresa M Allen; Cheryl L Santos; Jan Balzarini; Erik De Clercq
Cytotoxic mannich bases of 1-arylidene-2-tetralones.
Journal of enzyme inhibition and medicinal chemistry 2003;18(4):313-24.
2003: Cristina Mazzon; Chiara Rampazzo; Maria Chiara Scaini; Lisa Gallinaro; Anna Karlsson; Chris Meier; Jan Balzarini; Peter Reichard; Vera Bianchi
Cytosolic and mitochondrial deoxyribonucleotidases: activity with substrate analogs, inhibitors and implications for therapy.
Biochemical pharmacology 2003;66(3):471-9.
2003: Yongseok Choi; Clifford George; Maria J Comin; Joseph J Barchi; Hak-Sung Kim; Kenneth Alan Jacobson; Jan Balzarini; Hiroaki Mitsuya; Paul L Boyer; Stephen H Hughes; Victor E Marquez
A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude.
Journal of medicinal chemistry 2003;46(15):3292-9.
2003: Louise Bird; Jingshan Ren; Alan Wright; Kris D Leslie; Bart Degrève; Jan Balzarini; David K Stammers
Crystal structure of varicella zoster virus thymidine kinase.
The Journal of biological chemistry 2003;278(27):24680-7.
2003: Stefano Manfredini; Nicola Solaroli; Angela Angusti; Federico Nalin; Elisa Durini; Silvia Vertuani; Pricl Sabrina; Marco Ferrone; Silvio Spadari; Federico Focher; Annalisa Verri; Erik De Clercq; Jan Balzarini
Design and synthesis of phosphonoacetic acid (PPA) ester and amide bioisosters of ribofuranosylnucleoside diphosphates as potential ribonucleotide reductase inhibitors and evaluation of their enzyme inhibitory, cytostatic and antiviral activity.
Antiviral chemistry & chemotherapy 2003;14(4):183-94.
2003: Christophe Galtier; Sylvie Mavel; Robert Snoeck; Graciela Andreï; Christophe Pannecouque; Myriam Witvrouw; Jan Balzarini; Erik De Clercq; Alain Gueiffier
Synthesis and antiviral activities of 3-aralkylthiomethylimidazo[1,2-b]pyridazine derivatives.
Antiviral chemistry & chemotherapy 2003;14(4):177-82.
2003: Ge Meng; Fen-Er Chen; Erik De Clercq; Jan Balzarini; Christophe Pannecouque
Nonnucleoside HIV-1 reverse transcriptase inhibitors: Part I. Synthesis and structure-activity relationship of 1-alkoxymethyl-5-alkyl-6-naphthylmethyl uracils as HEPT analogues.
Chemical & pharmaceutical bulletin 2003;51(7):779-89.
2003: Karoline Spaepen; Sigrid Stroobants; Patrick Dupont; Peter Vandenberghe; Johan Maertens; Guy Bormans; José Thomas; Jan Balzarini; Christiane De Wolf-Peeters; Luc Mortelmans; Gregor Verhoef
Prognostic value of pretransplantation positron emission tomography using fluorine 18-fluorodeoxyglucose in patients with aggressive lymphoma treated with high-dose chemotherapy and stem cell transplantation.
Blood 2003;102(1):53-9.
2003: Jan Balzarini; Christophe Pannecouque; Erik De Clercq; Andrey Y Pavlov; Svetlana S Printsevskaya; Olga V Miroshnikova; Marina I Reznikova; Maria N Preobrazhenskaya
Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics.
Journal of medicinal chemistry 2003;46(13):2755-64.
2003: Béatrice Roy; Stéphane Chambert; Michel Lepoivre; Anne-Marie Aubertin; Jan Balzarini; Jean-Luc Décout
Deoxyribonucleoside 2'- or 3'-mixed disulfides: prodrugs to target ribonucleotide reductase and/or to inhibit HIV reverse transcription.
Journal of medicinal chemistry 2003;46(13):2565-8.
2003: Leen De Bolle; Jan Balzarini; Erik De Clercq; Lieve Naesens
Characterization of the catalytic subunit of the human herpesvirus 6 (HHV-6) DNA polymerase expressed in an in vitro transcription/translation assay.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):999-1001.
2003: Rebecca Sienaert; Lieve Naesens; Andrea Brancale; Antonella Carangio; Graciela Andrei; Robert Snoeck; André B P van Kuilenburg; Erik De Clercq; Christopher McGuigan; Jan Balzarini
Metabolic and pharmacological characteristics of the bicyclic nucleoside analogues (BCNAs) as highly selective inhibitors of varicella-zoster virus (VZV).
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):995-7.
2003: Sonia De Castro; María-Jesús Pérez-Pérez; Esther Lobatón; Erik De Clercq; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
Unusual lability of 5'-O-tert-butyldimethylsilyl group on 4''-acyl TSAO derivatives.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):959-61.
2003: Eva-María Priego; Jesús Mendieta; Federico Gago; Jan Balzarini; Erik De Clercq; María-José Camarasa; María-Jesús Pérez-Pérez
Towards new thymidine phosphorylase/PD-ECGF inhibitors based on the transition state of the enzyme reaction.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):951-3.
2003: María-Cruz Bonache; Cristina Chamorro; Sonsoles Velázquez; Erik De Clercq; Jan Balzarini; María-José Camarasa; Ana San-Félix
N-3 substituted TSAO derivatives as a probe to explore the dimeric interface of HIV-1 reverse transcriptase.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):947-9.
2003: Antonella Carangio; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic nucleoside inhibitors of varicella-zoster virus: synthesis and biological evaluation of 2',3'-dideoxy-3'-fluoro and 2'-deoxy-xylo derivatives.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):935-7.
2003: Giovanna M Luoni; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic nucleoside inhibitors of varicella-zoster virus: 5'-chloro and 3'-chloro derivatives.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):931-3.
2003: Tomasz Goslinski; Grazyna Wenska; Bozenna Golankiewicz; Jan Balzarini; Erik De Clercq
Synthesis and fluorescent properties of 6-(4-biphenylyl)-3,9-dihydro-9-oxo-5H-imidazo[1,2-a]purine analogues of acyclovir and ganciclovir.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):911-4.
2003: Boris S Ermolinsky; Ekaterina V Efimtseva; Cyrill S Alexeev; Sergey N Mikhailov; Jan Balzarini; Erik De Clercq
Dinucleoside monophosphates containing AZT and 1-methyladenosine or 7-methylguanosine.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):853-5.
2003: Christian Ducho; Jan Balzarini; Chris Meier
Non-inhibition of acetylcholinesterase by cycloSal nucleotides.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):841-3.
2003: Chris Meier; Jürgen Renze; Jan Balzarini; Erik De Clercq
d4TMP delivery from 7-substituted cycloSal-d4TMPs.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):825-7.
2003: H C Müller; Chris Meier; Jan Balzarini; J Reinstein
Novel nucleotide analogues as potential substrates for TMPK, a key enzyme in the metabolism of AZT.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):821-3.
2003: Olivier Bidet; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Synthesis of unusual bicyclic nucleosides bearing an unsaturated side-chain, as potential inhibitors of varicella-zoster virus (VZV).
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):817-9.
2003: U Muus; Erik De Clercq; Jan Balzarini; Lieve Naesens; Chris Meier
Study of different substituted cyclic and acyclic benzylpronucleotides of d4T relative to their hydrolytic stability and antiviral activity.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):791-5.
2003: Vladimir N Barai; Anatoli I Zinchenko; Ludmilla A Eroshevskaya; Elena V Zhernosek; Jan Balzarini; Erik De Clercq; Igor Mikhailopulo
Chemo-enzymatic synthesis of 3-deoxy-beta-D-ribofuranosyl purines and study of their biological properties.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):751-3.
2003: Christopher McGuigan; Alison Jukes; Sally Blewett; Hubert Barucki; Jonathan T Erichsen; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Halophenyl furanopyrimidines as potent and selective anti-VZV agents.
Antiviral chemistry & chemotherapy 2003;14(3):165-70.
2003: Jan Balzarini; Erik De Clercq; Bozena Kaminska; Andrzej Orzeszko
Synthesis and antiviral activity of some 5'-N-phthaloyl-3'-azido-2',3'-dideoxythymidine analogues.
Antiviral chemistry & chemotherapy 2003;14(3):139-44.
2003: Jarek Poznanski; Maria Bretner; Tadeusz Kulikowski; Jan Balzarini; Arthur Van Aerschot; Erik De Clercq
Synthesis, solution conformation and anti-HIV activity of novel 3'-substituted-2',3'-dideoxy-5-hydroxymethyluridines and their 4,5-substituted analogues.
Antiviral chemistry & chemotherapy 2003;14(3):127-38.
2003: Glen Reid; peter wielinga; Noam Zelcer; Marcel de Haas; Liesbeth Van Deemter; Jan Wijnholds; Jan Balzarini; Piet Borst
Characterization of the transport of nucleoside analog drugs by the human multidrug resistance proteins MRP4 and MRP5.
Molecular pharmacology 2003;63(5):1094-103.
2003: Karoline Spaepen; Sigrid Stroobants; Patrick Dupont; Guy Bormans; Jan Balzarini; Gregor Verhoef; Luc Mortelmans; Peter Vandenberghe; Christiane De Wolf-Peeters
[(18)F]FDG PET monitoring of tumour response to chemotherapy: does [(18)F]FDG uptake correlate with the viable tumour cell fraction?
European journal of nuclear medicine and molecular imaging 2003;30(5):682-8.
2003: Riad Agbaria; Esther Manor; Jacob Barak; Jan Balzarini
Phosphorylation of 3'-azidothymidine in maternal and fetal peripheral blood mononuclear cells during gestation and at term.
Journal of acquired immune deficiency syndromes (1999) 2003;32(5):477-81.
2003: Irene M Lagoja; Christophe Pannecouque; Arthur Van Aerschot; Myriam Witvrouw; zeger debyser; Jan Balzarini; Piet Herdewijn; Erik De Clercq
N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action.
Journal of medicinal chemistry 2003;46(8):1546-53.
2003: Zoran Dzolić; Vedran Kristafor; Mario Cetina; Ante Nagl; Antonija Hergold-Brundić; Draginja Mrvos-Sermek; Thomas Burgemeister; Mira Grdisa; Neda Slade; Kresimir Pavelić; Jan Balzarini; Erik De Clercq; Mladen Mintas
Synthesis, structural studies, and biological evaluation of some purine substituted 1-aminocyclopropane-1-carboxylic acids and 1-amino-1-hydroxymethylcyclopropanes.
Nucleosides, nucleotides & nucleic acids 2003;22(4):373-89.
2003: Jonathan R Dimmock; Amitabh Jha; Gordon A Zello; Theresa M Allen; Cheryl L Santos; Jan Balzarini; Erik De Clercq; Elias K Manavathu; James P Stables
Cytotoxic 4'-aminochalcones and related compounds.
Die Pharmazie 2003;58(4):227-32.
2003: Ebrahim Naimi; Aihua Zhou; Panteha Khalili; Leonard I Wiebe; Jan Balzarini; Erik De Clercq; Edward E Knaus
Synthesis of 3'- and 5'-nitrooxy pyrimidine nucleoside nitrate esters: "nitric oxide donor" agents for evaluation as anticancer and antiviral agents.
Journal of medicinal chemistry 2003;46(6):995-1004.
2003: Jonathan R Dimmock; Maniyan Padmanilayam; Gordon A Zello; Kurt H Nienaber; Theresa M Allen; Cheryl L Santos; Erik De Clercq; Jan Balzarini; Elias K Manavathu; James P Stables
Cytotoxic analogues of 2,6-bis(arylidene)cyclohexanones.
European journal of medicinal chemistry 2003;38(2):169-77.
2003: Jan Balzarini; Ana-Isabel Hernández; Philippe Roche; Robert M Esnouf; Anna Karlsson; María-José Camarasa; María-Jesús Pérez-Pérez
Non-nucleoside inhibitors of mitochondrial thymidine kinase (TK-2) differentially inhibit the closely related herpes simplex virus type 1 TK and Drosophila melanogaster multifunctional deoxynucleoside kinase.
Molecular pharmacology 2003;63(2):263-70.
2002: Sven Guenther; Jan Balzarini; Erik De Clercq; Vasu Nair
A thymidine phosphorylase-stable analogue of BVDU with significant antiviral activity.
Journal of medicinal chemistry 2002;45(25):5426-9.
2002: Jonathan R Dimmock; Amitabh Jha; Gordon A Zello; J Wilson Quail; Eliud O Oloo; Kurt H Nienaber; Earl S Kowalczyk; Theresa M Allen; Cheryl L Santos; Erik De Clercq; Jan Balzarini; Elias K Manavathu; James P Stables
Cytotoxic N-[4-(3-aryl-3-oxo-1-propenyl)phenylcarbonyl]-3,5-bis(phenylmethylene)-4-piperidones and related compounds.
European journal of medicinal chemistry 2002;37(12):961-72.
2002: Maria Letizia Barreca; Jan Balzarini; Alba Chimirri; Erik De Clercq; Laura De Luca; Hans-Dieter Höltje; Monika Höltje; Anna Maria Monforte; Pietro Monforte; Christophe Pannecouque; Angela Rao; Maria Zappalà
Design, synthesis, structure-activity relationships, and molecular modeling studies of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV agents.
Journal of medicinal chemistry 2002;45(24):5410-3.
2002: Jan Balzarini; Yven Van Herrewege; Guido Vanham
Metabolic activation of nucleoside and nucleotide reverse transcriptase inhibitors in dendritic and Langerhans cells.
AIDS (London, England) 2002;16(16):2159-63.
2002: Tomasz Goslinski; Bozenna Golankiewicz; Erik De Clercq; Jan Balzarini
Synthesis and biological activity of strongly fluorescent tricyclic analogues of acyclovir and ganciclovir.
Journal of medicinal chemistry 2002;45(23):5052-7.
2002: Yven Van Herrewege; Lieve Penne; Chris Vereecken; Katrien Fransen; Guido van der Groen; Luc Kestens; Jan Balzarini; Guido Vanham
Activity of reverse transcriptase inhibitors in monocyte-derived dendritic cells: a possible in vitro model for postexposure prophylaxis of sexual HIV transmission.
AIDS research and human retroviruses 2002;18(15):1091-102.
2002: Jonathan R Dimmock; Maniyan P Padmanilyam; Gordon A Zello; J Wilson Quail; Eliud O Oloo; Jared S Prisciak; Heinz-Bernhard Kraatz; Arten Cherkasov; Jeremy S Lee; Theresa M Allen; Cheryl L Santos; Elias K Manavathu; Erik De Clercq; Jan Balzarini; James P Stables
Cytotoxic 1,3-diarylidene-2-tetralones and related compounds.
European journal of medicinal chemistry 2002;37(10):813-24.
2002: Chris Meiera; Jürgen Renzea; Christian Ducho; Jan Balzarini
cycloSal-d4TMP pronucleotides structural variations, mechanistic insights and antiviral activity.
Current topics in medicinal chemistry 2002;2(10):1111-21.
2002: Ana-Isabel Hernández; Jan Balzarini; Anna Karlsson; María-José Camarasa; María-Jesús Pérez-Pérez
Acyclic nucleoside analogues as novel inhibitors of human mitochondrial thymidine kinase.
Journal of medicinal chemistry 2002;45(19):4254-63.
2002: Antonella Carangio; Sheila Srinivasan; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic nucleoside inhibitors of varicella-zoster virus: effect of terminal aryl substitution in the side-chain.
Antiviral chemistry & chemotherapy 2002;13(5):263-71.
2002: Lourdes Santana; Marta Teijeira; Eugenio Uriarte; Jan Balzarini; Erik De Clercq
Synthesis, conformational analysis and antiviral and antitumoral activity of new 1,2-disubstituted carbocyclic nucleosides.
European journal of medicinal chemistry 2002;37(9):755-60.
2002: Jan Balzarini; Tomasz Ostrowski; Tomasz Goslinski; Erik De Clercq; Bozenna Golankiewicz
Pronounced cytostatic activity and bystander effect of a novel series of fluorescent tricyclic acyclovir and ganciclovir derivatives in herpes simplex virus thymidine kinase gene-transduced tumor cell lines.
Gene therapy 2002;9(17):1173-82.
2002: Esther Lobatón; Fátima Rodríguez-Barrios; Federico Gago; María-Jesús Pérez-Pérez; Erik De Clercq; Jan Balzarini; María-José Camarasa; Sonsoles Velázquez
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach.
Journal of medicinal chemistry 2002;45(18):3934-45.
2002: Stefano Aquaro; Raffaele Caliò; Jan Balzarini; Maria Concetta Bellocchi; Enrico Garaci; Carlo Federico Perno
Macrophages and HIV infection: therapeutical approaches toward this strategic virus reservoir.
Antiviral research 2002;55(2):209-25.
2002: Jan Balzarini; Christopher McGuigan
Chemotherapy of varicella-zoster virus by a novel class of highly specific anti-VZV bicyclic pyrimidine nucleosides.
Biochimica et biophysica acta 2002;1587(2-3):287-95.
2002: Jonathan R Dimmock; Gordon A Zello; Eliud O Oloo; J Wilson Quail; Heinz-Bernhard Kraatz; Pal Perjesi; Ferenc Aradi; Krisztina Takács-Novák; Theresa M Allen; Cheryl L Santos; Jan Balzarini; Erik De Clercq; James P Stables
Correlations between cytotoxicity and topography of some 2-arylidenebenzocycloalkanones determined by X-ray crystallography.
Journal of medicinal chemistry 2002;45(14):3103-11.
2002: Jan Balzarini; Christopher McGuigan
Bicyclic pyrimidine nucleoside analogues (BCNAs) as highly selective and potent inhibitors of varicella-zoster virus replication.
The Journal of antimicrobial chemotherapy 2002;50(1):5-9.
2002: Jan Balzarini; Christophe Pannecouque; Erik De Clercq; Stefano Aquaro; Carlo Federico Perno; Herman Egberink; Antonín Holý
Antiretrovirus activity of a novel class of acyclic pyrimidine nucleoside phosphonates.
Antimicrobial agents and chemotherapy 2002;46(7):2185-93.
2002: David T Manallack; William Pitt; Piet Herdewijn; Jan Balzarini; Erik De Clercq; Mark R Sanderson; Maninder Sohi; Frank Wien; Hélène Munier-Lehmann; Ahmed Haouz; Marc Delarue
Database searching for thymidine and thymidylate kinase inhibitors using three-dimensional structure-based methods.
Journal of enzyme inhibition and medicinal chemistry 2002;17(3):167-74.
2002: Jan Balzarini; Sandra Liekens; Robert M Esnouf; Erik De Clercq
The A167Y mutation converts the herpes simplex virus type 1 thymidine kinase into a guanosine analogue kinase.
Biochemistry 2002;41(20):6517-24.
2002: Jan Balzarini; Rebecca Sienaert; Sandra Liekens; André B P van Kuilenburg; Antonella Carangio; Robert M Esnouf; Erik De Clercq; Christopher McGuigan
Lack of susceptibility of bicyclic nucleoside analogs, highly potent inhibitors of varicella-zoster virus, to the catabolic action of thymidine phosphorylase and dihydropyrimidine dehydrogenase.
Molecular pharmacology 2002;61(5):1140-5.
2002: Antonín Holý; Ivan Votruba; Milena Masojídková; Graciela Andrei; Robert Snoeck; Lieve Naesens; Erik De Clercq; Jan Balzarini
6-[2-(Phosphonomethoxy)alkoxy]pyrimidines with antiviral activity.
Journal of medicinal chemistry 2002;45(9):1918-29.
2002: Sylvie Mavel; Jean-Louis Renou; Christophe Galtier; Hassan Allouchi; Robert Snoeck; Graciela Andrei; Erik De Clercq; Jan Balzarini; Alain Gueiffier
Influence of 2-substituent on the activity of imidazo[1,2-a] pyridine derivatives against human cytomegalovirus.
Bioorganic & medicinal chemistry 2002;10(4):941-6.
2002: Sven Deferme; Jan Van Gelder; Françoise M Ingels; Guy Van den Mooter; Stefan S De Buck; Jan Balzarini; Lieve Naesens; Erik De Clercq; Renaat Kinget; Patrick Augustijns
Intestinal absorption characteristics of the low solubility thiocarboxanilide UC-781.
International journal of pharmaceutics 2002;234(1-2):113-9.
2002: Christopher McGuigan; Sally Blewett; Dario Siccardi; Jonathan T Erichsen; Graciela Andrei; Robert Snoek; Erik De Clercq; Jan Balzarini
Alkyloxyphenyl furano pyrimidines as potent and selective anti-VZV agents with enhanced water solubility.
Antiviral chemistry & chemotherapy 2002;13(2):91-9.
2002: Christian Ducho; Jan Balzarini; Lieve Naesens; Erik De Clercq; Chris Meier
Aryl-substituted and benzo-annulated cyc/osal-derivatives of 2',3'-dideoxy-2',3'-didehydrothymidine monophosphate--correlation of structure, hydrolysis properties and anti-HIV activity.
Antiviral chemistry & chemotherapy 2002;13(2):129-41.
2002: Chris Meier; Ulrike Muus; Jürgen Renze; Lieve Naesens; Erik De Clercq; Jan Balzarini
Comparative study of bis(benzyl)phosphate triesters of 2',3'-dideoxy-2',3'-didehydrothymidine (d4T) and cyclosal-d4TMP--hydrolysis, mechanistic insights and anti-HIV activity.
Antiviral chemistry & chemotherapy 2002;13(2):101-14.
2002: Joeri Auwerx; Thomas W North; Bradley D Preston; George J Klarmann; Erik De Clercq; Jan Balzarini
Chimeric human immunodeficiency virus type 1 and feline immunodeficiency virus reverse transcriptases: role of the subunits in resistance/sensitivity to non-nucleoside reverse transcriptase inhibitors.
Molecular pharmacology 2002;61(2):400-6.
2002: Rebecca Sienaert; Lieve Naesens; Andrea Brancale; Erik De Clercq; Christopher McGuigan; Jan Balzarini
Specific recognition of the bicyclic pyrimidine nucleoside analogs, a new class of highly potent and selective inhibitors of varicella-zoster virus (VZV), by the VZV-encoded thymidine kinase.
Molecular pharmacology 2002;61(2):249-54.
2002: Subha R Das; Stewart W Schneller; Jan Balzarini; Erik De Clercq
A mercapto analogue of 5'-noraristeromycin.
Bioorganic & medicinal chemistry 2002;10(2):457-60.
2002: Sandra Liekens; Filip Bilsen; Erik De Clercq; Eva-María Priego; María-José Camarasa; María-Jesús Pérez-Pérez; Jan Balzarini
Anti-angiogenic activity of a novel multi-substrate analogue inhibitor of thymidine phosphorylase.
FEBS letters 2002;510(1-2):83-8.
2002: Jörn Wirsching; Oliver Schulze; Jürgen Voss; Anja Giesler; Jürgen Kopf; Gunadi Adiwidjaja; Jan Balzarini; Erik De Clercq
Synthesis and biological evaluation of isonucleosides derived from methyl 3,5-anhydro-2-O-(2-fluorobenzyl)-D-xylofuranosides.
Nucleosides, nucleotides & nucleic acids 2002;21(3):257-74.
2002: M Isabel Nieto; Olga Caamaño; Franco Fernández; Maria Gómez; Jan Balzarini; Erik De Clercq
Synthesis, antiviral and cytostatic activities, of carbocyclic nucleosides incorporating a modified cyclopentane ring. IV. Adenosine and uridine analogues.
Nucleosides, nucleotides & nucleic acids 2002;21(3):243-55.
2002: Jean M J Tronchet; Frederic Chalard; Elisabeth Rivara-Minten; Michel Seman; Erik De Clercq; Jan Balzarini; Pierre J Dilda
Synthesis and in vitro cytotoxic and antiviral activities of 1-(2,5,6-trideoxy-6-halogenohept-5-enofuranurononitrile)thymine and derivatives.
Nucleosides, nucleotides & nucleic acids 2002;21(3):191-206.
2002: Jonathan R Dimmock; Amitabh Jha; Praveen Kumar; Gordon A Zello; J Wilson Quail; Eliud O Oloo; Jennifer J Oucharek; Mohammed Khysar Pasha; Dallas P Seitz; Rajendra K Sharma; Theresa M Allen; Cheryl L Santos; Elias K Manavathu; Erik De Clercq; Jan Balzarini; James P Stables
Cytotoxic 1,4-bis(2-oxo-1-cycloalkylmethylene)benzenes and related compounds.
European journal of medicinal chemistry 2002;37(1):35-44.
2001: Cristina Chamorro; Esther Lobatón; María-Cruz Bonache; Erik De Clercq; Jan Balzarini; Sonsoles Velázquez; Ana San-Félix; María-José Camarasa
Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.
Bioorganic & medicinal chemistry letters 2001;11(23):3085-8.
2001: Jean M J Tronchet; I Kovacs; Pierre J Dilda; Michel Seman; G Andrei; R Snoeck; Erik De Clercq; Jan Balzarini
Synthesis and anti-HIV activity of thymidine analogues bearing a 4'-cyanovinyl group and some derivatives thereof.
Nucleosides, nucleotides & nucleic acids 2001;20(12):1927-39.
2001: A Chaouni-Enabdallah; Christophe Galtier; Hassan Allouchi; A Kherbeche; Olivier Chavignon; Jean-Claude Teulade; Myriam Witvrouw; Christophe Pannecouque; Robert Snoeck; Graciela Andrei; Jan Balzarini; Erik De Clercq; Florence Fauvelle; Cécile Enguehard; Alain Gueiffier
3-Benzamido, ureido and thioureidoimidazo[1,2-a]pyridine derivatives as potential antiviral agents.
Chemical & pharmaceutical bulletin 2001;49(12):1631-5.
2001: Jan Balzarini; Erik De Clercq
Rapid alternation of drug therapy is highly efficient in suppressing the emergence of mutant drug-resistant HIV strains in cell culture.
AIDS research and human retroviruses 2001;17(17):1625-34.
2001: Ana Martinez; Carmen Gil; Ana Castro; Concepción Perez; M Witvrouw; C Pannecouque; Jan Balzarini; Erik De Clercq
Anti-HIV-1 activity of benzothiadiazine dioxide.
Antiviral chemistry & chemotherapy 2001;12(6):347-51.
2001: Karoline Spaepen; Sigrid Stroobants; Patrick Dupont; José Thomas; Peter Vandenberghe; Jan Balzarini; Christiane De Wolf-Peeters; Luc Mortelmans; Gregor Verhoef
Can positron emission tomography with [(18)F]-fluorodeoxyglucose after first-line treatment distinguish Hodgkin's disease patients who need additional therapy from others in whom additional therapy would mean avoidable toxicity?
British journal of haematology 2001;115(2):272-8.
2001: Andrea Brancale; Christopher McGuigan; B Algain; Pascal Savy; Rachid Benhida; Jean-Louis Fourrey; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic anti-VZV nucleosides: Thieno analogues retain full antiviral activity.
Bioorganic & medicinal chemistry letters 2001;11(18):2507-10.
2001: Jan Balzarini; F Haller-Meier; Erik De Clercq; C Meier
Antiviral activity of cyclosaligenyl prodrugs of acyclovir, carbovir and abacavir.
Antiviral chemistry & chemotherapy 2001;12(5):301-6.
2001: Sarah A Harris; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Synthesis and antiviral evaluation of phosphoramidate derivatives of (E)-5-(2-bromovinyl)-2'-deoxyuridine.
Antiviral chemistry & chemotherapy 2001;12(5):293-300.
2001: Jörn Wirsching; Jürgen Voss; Gunadi Adiwidjaja; Jan Balzarini; Erik De Clercq
Thiosugars. VIII. Preparation of new 4'-thio-L-lyxo pyrimidine nucleoside analogues.
Nucleosides, nucleotides & nucleic acids 2001;20(9):1625-45.
2001: H Pelemans; Robert M Esnouf; K L Min; Michael A Parniak; Erik De Clercq; Jan Balzarini
Mutations at amino acid positions 63, 189, and 396 of human immunodeficiency virus type 1 reverse transcriptase (RT) partially restore the DNA polymerase activity of a Trp229Tyr mutant RT.
Virology 2001;287(1):143-50.
2001: Pier Giovanni Baraldi; Gianfranco Balboni; Maria Giovanna Pavani; Giampiero Spalluto; Mojgan Aghazadeh Tabrizi; E D Clercq; Jan Balzarini; T Bando; H Sugiyama; LUISA-CARLOTA LÓPEZ-CARA
Design, synthesis, DNA binding, and biological evaluation of water-soluble hybrid molecules containing two pyrazole analogues of the alkylating cyclopropylpyrroloindole (CPI) subunit of the antitumor agent CC-1065 and polypyrrole minor groove binders.
Journal of medicinal chemistry 2001;44(16):2536-43.
2001: Festo Damian; Norbert Blaton; HO Desseyn; K Clou; Patrick Augustijns; Lieve Naesens; Jan Balzarini; Renaat Kinget; Guy Van den Mooter
Solid state properties of pure UC-781 and solid dispersions with polyvinylpyrrolidone (PVP K30).
The Journal of pharmacy and pharmacology 2001;53(8):1109-16.
2001: Maria Letizia Barreca; Alba Chimirri; Laura De Luca; Anna Maria Monforte; Pietro Monforte; Angela Rao; Maria Zappalà; Jan Balzarini; Erik De Clercq; Christophe Pannecouque; Myriam Witvrouw
Discovery of 2,3-diaryl-1,3-thiazolidin-4-ones as potent anti-HIV-1 agents.
Bioorganic & medicinal chemistry letters 2001;11(13):1793-6.
2001: A Chaouni-Benabdallah; Christophe Galtier; Hassan Allouchi; A Kherbeche; Jean-Claude Debouzy; Jean-Claude Teulade; Olivier Chavignon; Myriam Witvrouw; Christophe Pannecouque; Jan Balzarini; Erik De Clercq; Cécile Enguehard; Alain Gueiffier
Synthesis of 3-nitrosoimidazo[1,2-a]pyridine derivatives as potential antiretroviral agents.
Archiv der Pharmazie 2001;334(7):224-8.
2001: Jan Balzarini; María-José Camarasa; María-Jesús Pérez-Pérez; Ana San-Félix; Sonsoles Velázquez; Carlo Federico Perno; Erik De Clercq; J N Anderson; Anna Karlsson
Exploitation of the low fidelity of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase and the nucleotide composition bias in the HIV-1 genome to alter the drug resistance development of HIV.
Journal of virology 2001;75(13):5772-7.
2001: Fátima Rodríguez-Barrios; C Pérez; Esther Lobatón; Sonsoles Velázquez; Cristina Chamorro; Ana San-Félix; María-Jesús Pérez-Pérez; María-José Camarasa; H Pelemans; Jan Balzarini; Federico Gago
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase.
Journal of medicinal chemistry 2001;44(12):1853-65.
2001: Cristina Chamorro; María-Jesús Pérez-Pérez; Fátima Rodríguez-Barrios; Federico Gago; Erik De Clercq; Jan Balzarini; Ana San-Félix; María-José Camarasa
Exploring the role of the 5'-position of TSAO-T. Synthesis and anti-HIV evaluation of novel TSAO-T derivatives.
Antiviral research 2001;50(3):207-22.
2001: Stefano Manfredini; Pier Giovanni Baraldi; Elisa Durini; L Porcu; Angela Angusti; Silvia Vertuani; Nicola Solaroli; Erik De Clercq; Anna Karlsson; Jan Balzarini
Design, synthesis and enzymatic activity of highly selective human mitochondrial thymidine kinase inhibitors.
Bioorganic & medicinal chemistry letters 2001;11(10):1329-32.
2001: Antonella Carangio; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic nucleoside inhibitors of varicella-zoster virus (VZV): Pd-catalysed synthesis of 5-aryl derivatives and their biological evaluation.
Antiviral chemistry & chemotherapy 2001;12(3):187-97.
2001: Alba Chimirri; Pietro Monforte; Angela Rao; Maria Zappalà; Anna Maria Monforte; G De Sarro; Christophe Pannecouque; Myriam Witvrouw; Jan Balzarini; Erik De Clercq
Synthesis, biological activity, pharmacokinetic properties and molecular modelling studies of novel 1H,3H-oxazolo[3,4-a]benzimidazoles: non-nucleoside HIV-1 reverse transcriptase inhibitors.
Antiviral chemistry & chemotherapy 2001;12(3):169-74.
2001: C Ballatore; Christopher McGuigan; Erik De Clercq; Jan Balzarini
Synthesis and evaluation of novel amidate prodrugs of PMEA and PMPA.
Bioorganic & medicinal chemistry letters 2001;11(8):1053-6.
2001: Jörn Wirsching; Jürgen Voss; Gunadi Adiwidjaja; Jan Balzarini; Erik De Clercq
Thiosugars. Part 9: synthesis and biological evaluation of some 4'-thio-L-arabino nucleoside analogues.
Bioorganic & medicinal chemistry letters 2001;11(8):1049-51.
2001: Jürgen Renze; Martin Plath; Christian Ducho; Jan Balzarini; Erik De Clercq; Chris Meier
Benzyl-functionalized cycloSal-d4T monophosphates.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):931-4.
2001: Sheila Srinivasan; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic nucleoside inhibitors of varicella-zoster virus (VZV): effect of terminal unsaturation in the side-chain.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):763-6.
2001: C M Huntley; A S Cotterill; J Y Maillard; Jan Balzarini; Claire Simons
Synthesis and biological evaluation of pyridin-2-one nucleosides.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):731-3.
2001: Esther Lobatón; Sonsoles Velázquez; Ana San-Félix; Erik De Clercq; Jan Balzarini; María-José Camarasa
4"-H-TSAO-T, a novel prototype in the HIV-1 specific TSAO family.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):711-4.
2001: Esther Lobatón; Sonsoles Velázquez; María-Jesús Pérez-Pérez; María-Luisa Jimeno; Ana San-Félix; Erik De Clercq; Jan Balzarini; María-José Camarasa
"Second generation" of TSAO compounds directed against HIV-1 TSAO-resistant strains.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):707-10.
2001: Antonella Carangio; Christopher McGuigan; D Cahard; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Synthesis and in vitro evaluation of novel anti-varicella-zoster virus (VZV) nucleosides.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):653-6.
2001: Christopher McGuigan; Hubert Barucki; Antonella Carangio; Sally Blewett; Sheila Srinivasan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Novel aryl substituted bicyclic furo nucleosides as extremely potent and selective anti-VZV agents.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):287-96.
2001: Erik De Clercq; Graciela Andrei; Robert Snoeck; Leen De Bolle; Lieve Naesens; B Degrève; Jan Balzarini; Ying Zhang; Dominique Schols; Pieter Leyssen; Chunxiao Ying; Johan Neyts
Acyclic/carbocyclic guanosine analogues as anti-herpesvirus agents.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):271-85.
2001: Olga Caamaño; María José Figueira; Franco Fernández; Marcos García; M Isabel Nieto; Erik De Clercq; Jan Balzarini
Synthesis and evaluation of antiviral activity of higher homologues of xylo-carbocyclic nucleosides.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):1137-9.
2001: Sally Blewett; Christopher McGuigan; Hubert Barucki; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic furo pyrimidine nucleosides with aryloxyphenyl and halophenyl substituted side chains as potent and selective varicella-zoster virus inhibitors.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):1063-6.
2001: Kristel Van Laethem; Myriam Witvrouw; Christophe Pannecouque; Barbara Van Remoortel; Jean-Claude Schmit; Robert M Esnouf; JP Kleim; Jan Balzarini; Jan Desmyter; Erik De Clercq; Anne-Mieke Vandamme
Mutations in the non-nucleoside binding-pocket interfere with the multi-nucleoside resistance phenotype.
AIDS (London, England) 2001;15(5):553-61.
2001: Christopher McGuigan; Andrea Brancale; Hubert Barucki; Sheila Srinivasan; G Jones; Ranjith N Pathirana; Antonella Carangio; Sally Blewett; G Luoni; Olivier Bidet; A Jukes; C Jarvis; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Furano pyrimidines as novel potent and selective anti-VZV agents.
Antiviral chemistry & chemotherapy 2001;12(2):77-89.
2001: Subha R Das; Stewart W Schneller; Jan Balzarini; Erik De Clercq
5'-Nor carbocyclic 5'-deoxy-5'-(isobutylthio)adenosine and a 2',3'-dideoxy-2',3'-didehydro derivative.
Antiviral chemistry & chemotherapy 2001;12(2):119-24.
2001: Jonathan R Dimmock; Maniyan Padmanilayam; R N Puthucode; Adil J Nazarali; NL Motaganahalli; Gordon A Zello; J Wilson Quail; Eliud O Oloo; Heinz-Bernhard Kraatz; Jared S Prisciak; Theresa M Allen; Cheryl L Santos; Jan Balzarini; Erik De Clercq; Elias K Manavathu
A conformational and structure-activity relationship study of cytotoxic 3,5-bis(arylidene)-4-piperidones and related N-acryloyl analogues.
Journal of medicinal chemistry 2001;44(4):586-93.
2001: Sheila Srinivasan; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic nucleoside inhibitors of Varicella-Zoster Virus (VZV): the effect of terminal unsaturation in the side chain.
Bioorganic & medicinal chemistry letters 2001;11(3):391-3.
2001: H Pelemans; A Aertsen; Kristel Van Laethem; Anne-Mieke Vandamme; Erik De Clercq; María-Jesús Pérez-Pérez; Ana San-Félix; Sonsoles Velázquez; María-José Camarasa; Jan Balzarini
Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138.
Virology 2001;280(1):97-106.
2001: Karoline Spaepen; Sigrid Stroobants; Patrick Dupont; S Van Steenweghen; José Thomas; Peter Vandenberghe; L Vanuytsel; Guy Bormans; Jan Balzarini; Christiane De Wolf-Peeters; Luc Mortelmans; Gregor Verhoef
Prognostic value of positron emission tomography (PET) with fluorine-18 fluorodeoxyglucose ([18F]FDG) after first-line chemotherapy in non-Hodgkin's lymphoma: is [18F]FDG-PET a valid alternative to conventional diagnostic methods?
Journal of clinical oncology : official journal of the American Society of Clinical Oncology 2001;19(2):414-9.
2001: Achilleas Garoufis; Konstantina Karidi; N Hadjiliadis; S Kasselouri; J Kobe; Jan Balzarini; E De Clercq
Synthesis, Characterization and Antiviral Properties of Pd(II) Complexes With Penciclovir.
Metal-based drugs 2001;8(1):57-63.
2001: Sylvie Mavel; Jean-Louis Renou; Christophe Galtier; Robert Snoeck; Graciela Andrei; Jan Balzarini; Erik De Clercq; Alain Gueiffier
Synthesis of imidazo[1,2-a]pyridine derivatives as antiviral agents.
Arzneimittel-Forschung 2001;51(4):304-9.
2001: ZX Wang; Weili Duan; Leonard I Wiebe; Jan Balzarini; Erik De Clercq; Edward E Knaus
Synthesis of 1-(2-deoxy-beta-D-ribofuranosyl)-2,4-difluoro-5-substituted-benzenes: "thymine replacement" analogs of thymidine for evaluation as anticancer and antiviral agents.
Nucleosides, nucleotides & nucleic acids 2001;20(1-2):41-58.
2001: ZX Wang; Weili Duan; Leonard I Wiebe; Jan Balzarini; Erik De Clercq; Edward E Knaus
Synthesis of 1-(2-deoxy-beta-D-ribofuranosyl)-2,4-difluoro-5-substituted-benzene thymidine mimics, some related alpha-anomers, and their evaluation as antiviral and anticancer agents.
Nucleosides, nucleotides & nucleic acids 2001;20(1-2):11-40.
2000: Z X Wang; L I Wiebe; Jan Balzarini; Erik De Clercq; E E Knaus
Chiral synthesis of 4-[1-(2-deoxy-beta-L-ribofuranosyl)] derivatives of 2-substituted 5-fluoroaniline: "cytosine replacement" analogues of deoxy-beta-L-cytidine.
The Journal of organic chemistry 2000;65(26):9214-9.
2000: Christopher McGuigan; Hubert Barucki; Antonella Carangio; Sally Blewett; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini; Jonathan T Erichsen
Highly potent and selective inhibition of varicella-zoster virus by bicyclic furopyrimidine nucleosides bearing an aryl side chain.
Journal of medicinal chemistry 2000;43(26):4993-7.
2000: S Raić-Malić; D Svedruzić; Tatjana Gazivoda; A Marunović; A Hergold-Brundić; Ante Nagl; Jan Balzarini; Erik De Clercq; Mladen Mintas
Synthesis and antitumor activities of novel pyrimidine derivatives of 2,3-O,O-dibenzyl-6-deoxy-L-ascorbic acid and 4,5-didehydro-5,6- dideoxy-L-ascorbic acid.
Journal of medicinal chemistry 2000;43(25):4806-11.
2000: Andrea Brancale; Sheila Srinivasan; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Synthesis and anti-varicella-zoster virus activity of some novel bicyclic nucleoside inhibitors: effect of enhanced aqueous solubility.
Antiviral chemistry & chemotherapy 2000;11(6):383-93.
2000: Jonathan R Dimmock; Praveen Kumar; Adil J Nazarali; NL Motaganahalli; TP Kowalchuk; MA Beazely; J Wilson Quail; Eliud O Oloo; Theresa M Allen; J Szydlowski; E DeClercq; Jan Balzarini
Cytotoxic 2,6-bis(arylidene)cyclohexanones and related compounds.
European journal of medicinal chemistry 2000;35(11):967-77.
2000: Jan Balzarini; Stefano Aquaro; T Knispel; Chiara Rampazzo; Vera Bianchi; Carlo Federico Perno; Erik De Clercq; Chris Meier
Cyclosaligenyl-2',3'-didehydro-2',3'-dideoxythymidine monophosphate: efficient intracellular delivery of d4TMP.
Molecular pharmacology 2000;58(5):928-35.
2000: Jan Balzarini; B Degrève; A Esteban-Gamboa; Robert M Esnouf; Erik De Clercq; Yves Engelborghs; María-José Camarasa; María-Jesús Pérez-Pérez
Kinetic analysis of novel multisubstrate analogue inhibitors of thymidine phosphorylase.
FEBS letters 2000;483(2-3):181-5.
2000: Jonathan R Dimmock; NM Kandepu; Adil J Nazarali; NL Motaganahalli; TP Kowalchuk; U Pugazhenthi; Jared S Prisciak; J Wilson Quail; Theresa M Allen; R LeClerc; Cheryl L Santos; Erik De Clercq; Jan Balzarini
Sequential cytotoxicity: a theory evaluated using novel 2-[4-(3-aryl-2-propenoyloxy)phenylmethylene]cyclohexanones and related compounds.
Journal of medicinal chemistry 2000;43(21):3933-40.
2000: Jan Balzarini; C Zhu; Erik De Clercq; María-Jesús Pérez-Pérez; Cristina Chamorro; María-José Camarasa; A Karlsson
Novel ribofuranosylnucleoside lead compounds for potent and selective inhibitors of mitochondrial thymidine kinase-2.
The Biochemical journal 2000;351(Pt 1):167-71.
2000: Michael Knaggs; Christopher McGuigan; Sarah A Harris; P Heshmati; D Cahard; Ian H Gilbert; Jan Balzarini
A QSAR study investigating the effect of L-alanine ester variation on the anti-HIV activity of some phosphoramidate derivatives of d4T.
Bioorganic & medicinal chemistry letters 2000;10(18):2075-8.
2000: Christopher McGuigan; Ranjith N Pathirana; G Jones; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Anti-varicella-zoster virus bicyclic nucleosides: replacement of furo by pyrro base reduces antiviral potency.
Antiviral chemistry & chemotherapy 2000;11(5):343-8.
2000: ZX Wang; Weili Duan; Leonard I Wiebe; Erik De Clercq; Jan Balzarini; Edward E Knaus
Syntheses of 1-[(2-hydroxyethoxy)methyl]- and 1-[(1,3-dihydroxy-2-propoxy)methyl]- derivatives of 5-substituted-2,4-difluorobenzene: unnatural acyclo thymidine mimics for evaluation as anticancer and antiviral agents.
Nucleosides, nucleotides & nucleic acids 2000;19(9):1397-411.
2000: Ana Martinez; Carmen Gil; Concepción Perez; Ana Castro; C Prieto; Joaquin Otero; G Andrei; R Snoeck; Jan Balzarini; Erik De Clercq
Nonnucleoside human cytomegalovirus inhibitors: synthesis and antiviral evaluation of (chlorophenylmethyl)benzothiadiazine dioxide derivatives.
Journal of medicinal chemistry 2000;43(17):3267-73.
2000: Jan Balzarini
Effect of antimetabolite drugs of nucleotide metabolism on the anti-human immunodeficiency virus activity of nucleoside reverse transcriptase inhibitors.
Pharmacology & therapeutics 2000;87(2-3):175-87.
2000: Jan Wijnholds; CA Mol; Liesbeth Van Deemter; Marcel de Haas; George L Scheffer; F Baas; Jos H Beijnen; Rik J Scheper; S Hatse; E De Clercq; Jan Balzarini; Piet Borst
Multidrug-resistance protein 5 is a multispecific organic anion transporter able to transport nucleotide analogs.
Proceedings of the National Academy of Sciences of the United States of America 2000;97(13):7476-81.
2000: Jörn Wirsching; Jürgen Voss; Jan Balzarini; Erik De Clercq
Thiosugars. Part 5: synthesis and biological activity of 1-(4-thio-L-arabinofuranosyl)-5-halopyrimidine nucleosides.
Bioorganic & medicinal chemistry letters 2000;10(12):1339-41.
2000: Kristel Van Laethem; Jean-Claude Schmit; H Pelemans; Jan Balzarini; Myriam Witvrouw; María-Jesús Pérez-Pérez; María-José Camarasa; Robert M Esnouf; Stefano Aquaro; Alessandra Cenci; Carlo Federico Perno; Philippe Hermans; S Sprecher; Lidia Ruiz; Bonaventura Clotet; Eric Van Wijngaerden; Marc Van Ranst; Jan Desmyter; Erik De Clercq; Anne-Mieke Vandamme
Presence of 2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5"-(4"-amino-1",2"-oxath iole-2",2"-dioxide) (TSAO)-resistant virus strains in TSAO-inexperienced HIV patients.
AIDS research and human retroviruses 2000;16(9):825-33.
2000: Andrea Brancale; Christopher McGuigan; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Bicyclic nucleoside inhibitors of Varicella-Zoster Virus (VZV): the effect of a terminal halogen substitution in the side-chain.
Bioorganic & medicinal chemistry letters 2000;10(11):1215-7.
2000: H Pelemans; Robert M Esnouf; Erik De Clercq; Jan Balzarini
Mutational analysis of trp-229 of human immunodeficiency virus type 1 reverse transcriptase (RT) identifies this amino acid residue as a prime target for the rational design of new non-nucleoside RT inhibitors.
Molecular pharmacology 2000;57(5):954-60.
2000: Jan Balzarini; Erik De Clercq; An Carbonez; V Burt; JP Kleim
Long-term exposure of HIV type 1-infected cell cultures to combinations of the novel quinoxaline GW420867X with lamivudine, abacavir, and a variety of nonnucleoside reverse transcriptase inhibitors.
AIDS research and human retroviruses 2000;16(6):517-28.
2000: Jean M J Tronchet; I Kovacs; Michel Seman; Pierre J Dilda; Erik De Clercq; Jan Balzarini
Highly stereoselective synthesis and biological properties of nucleoside analogues bearing a spiro inserted oxirane ring.
Nucleosides, nucleotides & nucleic acids 2000;19(4):775-94.
2000: Jan Balzarini; B Degrève; Sigrid Hatse; Erik De Clercq; Michael Breuer; M Johansson; Roger Huybrechts; Anna Karlsson
The multifunctional deoxynucleoside kinase of insect cells is a target for the development of new insecticides.
Molecular pharmacology 2000;57(4):811-9.
2000: Kristel Van Laethem; Myriam Witvrouw; Jan Balzarini; Jean-Claude Schmit; S Sprecher; Philippe Hermans; M Leal; Thomas Harrer; Lidia Ruiz; Bonaventura Clotet; Marc Van Ranst; Jan Desmyter; Erik De Clercq; Anne-Mieke Vandamme
Patient HIV-1 strains carrying the multiple nucleoside resistance mutations are cross-resistant to abacavir.
AIDS (London, England) 2000;14(4):469-71.
2000: A Esteban-Gamboa; Jan Balzarini; Robert M Esnouf; Erik De Clercq; María-José Camarasa; María-Jesús Pérez-Pérez
Design, synthesis, and enzymatic evaluation of multisubstrate analogue inhibitors of Escherichia coli thymidine phosphorylase.
Journal of medicinal chemistry 2000;43(5):971-83.
2000: Christopher McGuigan; L Bidois; A Hiouni; C Ballatore; Erik De Clercq; Jan Balzarini
Phosphoramidate derivatives of stavudine as inhibitors of HIV: unnatural amino acids may substitute for alanine.
Antiviral chemistry & chemotherapy 2000;11(2):111-6.
2000: Jingshan Ren; Jonathan M Diprose; J Warren; Robert M Esnouf; Louise Bird; S Ikemizu; M Slater; John Milton; Jan Balzarini; David I Stuart; David K Stammers
Phenylethylthiazolylthiourea (PETT) non-nucleoside inhibitors of HIV-1 and HIV-2 reverse transcriptases. Structural and biochemical analyses.
The Journal of biological chemistry 2000;275(8):5633-9.
2000: Adam Siddiqui; Christopher McGuigan; C Ballatore; Sheila Srinivasan; Erik De Clercq; Jan Balzarini
Enhancing the aqueous solubility of d4T-based phosphoramidate prodrugs.
Bioorganic & medicinal chemistry letters 2000;10(4):381-4.
2000: Festo Damian; Norbert Blaton; Lieve Naesens; Jan Balzarini; Renaat Kinget; Patrick Augustijns; Guy Van den Mooter
Physicochemical characterization of solid dispersions of the antiviral agent UC-781 with polyethylene glycol 6000 and Gelucire 44/14.
European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences 2000;10(4):311-22.
2000: Cristina Chamorro; Erik De Clercq; Jan Balzarini; María-José Camarasa; Ana San-Félix
TSAO-T analogues bearing amino acids at position N-3 of thymine: synthesis and anti-human immunodeficiency virus activity.
Antiviral chemistry & chemotherapy 2000;11(1):61-9.
2000: Stefano Aquaro; O Wedgwood; CJ Yarnold; D Cahard; R Pathinara; Christopher McGuigan; R Calio'; Erik De Clercq; Jan Balzarini; Carlo Federico Perno
Activities of masked 2',3'-dideoxynucleoside monophosphate derivatives against human immunodeficiency virus in resting macrophages.
Antimicrobial agents and chemotherapy 2000;44(1):173-7.
1999: Sonsoles Velázquez; V Tuñón; María-Luisa Jimeno; Cristina Chamorro; Erik De Clercq; Jan Balzarini; María-José Camarasa
Potential multifunctional inhibitors of HIV-1 reverse transcriptase. Novel [AZT]-[TSAO-T] and [d4T]-[TSAO-T] heterodimers modified in the linker and in the dideoxynucleoside region.
Journal of medicinal chemistry 1999;42(25):5188-96.
1999: M E Arranz; JA Díaz; ST Ingate; Myriam Witvrouw; Christophe Pannecouque; Jan Balzarini; Erik De Clercq; S Vega
Synthesis and anti-HIV activity of 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazines (TTDs): a new family of HIV-1 specific non-nucleoside reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry 1999;7(12):2811-22.
1999: Jan Balzarini; Lieve Naesens; Stefano Aquaro; T Knispel; Carlo Federico Perno; Erik De Clercq; Chris Meier
Intracellular metabolism of CycloSaligenyl 3'-azido-2', 3'-dideoxythymidine monophosphate, a prodrug of 3'-azido-2', 3'-dideoxythymidine (zidovudine).
Molecular pharmacology 1999;56(6):1354-61.
1999: Christopher McGuigan; CJ Yarnold; G Jones; Sonsoles Velázquez; Hubert Barucki; Andrea Brancale; Graciela Andrei; Robert Snoeck; Erik De Clercq; Jan Balzarini
Potent and selective inhibition of varicella-zoster virus (VZV) by nucleoside analogues with an unusual bicyclic base.
Journal of medicinal chemistry 1999;42(22):4479-84.
1999: B Degrève; Robert M Esnouf; Erik De Clercq; Jan Balzarini
Characterization of multiple nuclear localization signals in herpes simplex virus type 1 thymidine kinase.
Biochemical and biophysical research communications 1999;264(2):338-42.
1999: AQ Siddiqui; Christopher McGuigan; C Ballatore; Fabio Zuccotto; Ian H Gilbert; Erik De Clercq; Jan Balzarini
Design and synthesis of lipophilic phosphoramidate d4T-MP prodrugs expressing high potency against HIV in cell culture: structural determinants for in vitro activity and QSAR.
Journal of medicinal chemistry 1999;42(20):4122-8.
1999: M Isabel Nieto; J Manuel Blanco; Olga Caamaño; Franco Fernández; Xerardo García-Mera; Carmen López; Jan Balzarini; Erik De Clercq
Synthesis and antiviral activity of carbocyclic nucleosides incorporating a modified cyclopentane ring. Part 3: Adenosine and uridine analogues.
Nucleosides & nucleotides 1999;18(10):2253-63.
1999: Stefaan Wera; B Degrève; Jan Balzarini; Erik De Clercq; Johan M Thevelein; Johan Neyts
Budding yeast as a screening tool for discovery of nucleoside analogs for use in HSV-1 TK suicide-gene therapy.
BioTechniques 1999;27(4):772-4, 776-7.
1999: D Saboulard; Lieve Naesens; D Cahard; A Salgado; Ranjith N Pathirana; S Velazquez; Christopher McGuigan; Erik De Clercq; Jan Balzarini
Characterization of the activation pathway of phosphoramidate triester prodrugs of stavudine and zidovudine.
Molecular pharmacology 1999;56(4):693-704.
1999: AQ Siddiqui; Christopher McGuigan; C Ballatore; O Wedgwood; Erik De Clercq; Jan Balzarini
Simple mono-derivatisation of the aryl moiety of D4A and DDA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture.
Bioorganic & medicinal chemistry letters 1999;9(17):2555-60.
1999: G Inguaggiato; David Hughes; Erik De Clercq; Jan Balzarini; Claire Simons
Novel 6-azapyrimidine-2'-deoxy-4'-thionucleosides: synthesis, biological evaluation and conformational analysis.
Antiviral chemistry & chemotherapy 1999;10(5):241-9.
1999: José Manuel Blanco; Olga Caamaño; Franco Fernández; Xerardo García-Mera; Antonio Rodríguez Hergueta; Carmen López; José Enrique Rodríguez-Borges; Jan Balzarini; Erik De Clercq
Synthesis and antiviral and antineoplastic activities of some novel carbocyclic guanosine analogues with a cyclobutane ring.
Chemical & pharmaceutical bulletin 1999;47(9):1314-7.
1999: Stefano Manfredini; Pier Giovanni Baraldi; Elisa Durini; Silvia Vertuani; Jan Balzarini; Erik De Clercq; Anna Karlsson; V Buzzoni; L Thelander
5'-Phosphoramidates and 5'-diphosphates of 2'-O-allyl-beta-D-arabinofuranosyluracil, -cytosine, and -adenine: inhibition of ribonucleotide reductase.
Journal of medicinal chemistry 1999;42(17):3243-50.
1999: Sigrid Hatse; Erik De Clercq; Jan Balzarini
Role of antimetabolites of purine and pyrimidine nucleotide metabolism in tumor cell differentiation.
Biochemical pharmacology 1999;58(4):539-55.
1999: A Martínez; A I Esteban; A Herrero; Carmen Ochoa; G Andrei; R Snoeck; Jan Balzarini; Erik De Clercq
Imidazothiadiazine dioxides: synthesis and antiviral activity.
Bioorganic & medicinal chemistry 1999;7(8):1617-23.
1999: Sigrid Hatse; Lieve Naesens; Erik De Clercq; Jan Balzarini
N6-cyclopropyl-PMEDAP: a novel derivative of 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) with distinct metabolic, antiproliferative, and differentiation-inducing properties.
Biochemical pharmacology 1999;58(2):311-23.
1999: Alba Chimirri; Silvana Grasso; Pietro Monforte; Angela Rao; Maria Zappalà; Anna Maria Monforte; Christophe Pannecouque; Myriam Witvrouw; Jan Balzarini; Erik De Clercq
Synthesis and biological activity of novel 1H,3H-thiazolo[3,4-a]benzimidazoles: non-nucleoside human immunodeficiency virus type 1 reverse transcriptase inhibitors.
Antiviral chemistry & chemotherapy 1999;10(4):211-7.
1999: Jan Balzarini
Suppression of resistance to drugs targeted to human immunodeficiency virus reverse transcriptase by combination therapy.
Biochemical pharmacology 1999;58(1):1-27.
1999: Antonín Holý; J Günter; Hana Dvoráková; Milena Masojídková; Graciela Andrei; Robert Snoeck; Jan Balzarini; Erik De Clercq
Structure-antiviral activity relationship in the series of pyrimidine and purine N-[2-(2-phosphonomethoxy)ethyl] nucleotide analogues. 1. Derivatives substituted at the carbon atoms of the base.
Journal of medicinal chemistry 1999;42(12):2064-86.
1999: K Breistøl; Jan Balzarini; ML Sandvold; F Myhren; M Martinsen; Erik De Clercq; Oystein Fodstad
Antitumor activity of P-4055 (elaidic acid-cytarabine) compared to cytarabine in metastatic and s.c. human tumor xenograft models.
Cancer research 1999;59(12):2944-9.
1999: Jonathan R Dimmock; NM Kandepu; Adil J Nazarali; TP Kowalchuk; NL Motaganahalli; J Wilson Quail; P A Mykytiuk; Gerald F Audette; Lata Prasad; Pal Perjesi; Theresa M Allen; Cheryl L Santos; J Szydlowski; Erik De Clercq; Jan Balzarini
Conformational and quantitative structure-activity relationship study of cytotoxic 2-arylidenebenzocycloalkanones.
Journal of medicinal chemistry 1999;42(8):1358-66.
1999: Ana Martinez; A I Esteban; Ana Castro; Carmen Gil; S Conde; Graciela Andrei; Robert Snoeck; Jan Balzarini; Erik De Clercq
Novel potential agents for human cytomegalovirus infection: synthesis and antiviral activity evaluation of benzothiadiazine dioxide acyclonucleosides.
Journal of medicinal chemistry 1999;42(7):1145-50.
1999: Sonsoles Velázquez; V Tuñón; María-Luisa Jimeno; María-Jesús Pérez-Pérez; Ana San-Félix; Cristina Chamorro; Esther Lobatón; A Esteban-Gamboa; Erik De Clercq; Jan Balzarini; María-José Camarasa
Novel series of [ddN]-[TSAO-T] heterodimers as potential bi-functional inhibitors of HIV-1 RT. Studies in the linker and ddN region.
Nucleosides & nucleotides 1999;18(4-5):1029-30.
1999: Stefano Manfredini; Pier Giovanni Baraldi; Elisa Durini; Jan Balzarini; Erik De Clercq; Anna Karlsson; V Buzzoni; L Thelander
Synthesis, cytostatic activity and inhibition of ribonucleotide reductase by 5'-phosphoramidates and 5'-diphosphates, of 2'-O-allyl-arabinofuranosyl nucleosides.
Nucleosides & nucleotides 1999;18(4-5):1007-8.
1999: R Bazzanini; Stefano Manfredini; Elisa Durini; Bettina Gröschel; Jindrich Cinatl; Jan Balzarini; Erik De Clercq; JL Imbach; Christian Périgaud; Gilles Gosselin
Prodrugs of Ara-CMP and Ara-AMP with a S-acyl-2-thioethyl (SATE) biolabile phosphate protecting group: synthesis and biological evaluation.
Nucleosides & nucleotides 1999;18(4-5):971-2.
1999: C Ballatore; Christopher McGuigan; Erik De Clercq; Jan Balzarini
An in situ pig liver esterase assay as a useful predictive tool for the likely in vitro anti viral activity of phosphoramidate pro-drugs.
Nucleosides & nucleotides 1999;18(4-5):967-9.
1999: Chris Meier; T Knispel; V E Marquez; Erik De Clercq; Jan Balzarini
CycloSal-2'-ara(ribo)-fluoro-2',3'-dideoxyadenosine monophosphates--an effort to solve the structure-activity relationship of 2'-fluoro-ddA.
Nucleosides & nucleotides 1999;18(4-5):907-12.
1999: Erik De Clercq; Graciela Andrei; Jan Balzarini; Sigrid Hatse; Sandra Liekens; Lieve Naesens; Johan Neyts; Robert Snoeck
Antitumor potential of acyclic nucleoside phosphonates.
Nucleosides & nucleotides 1999;18(4-5):759-71.
1999: Lourdes Santana; Marta Teijeira; Eugenio Uriarte; Carmen Terán; G Andrei; R Snoeck; Jan Balzarini; Erik De Clercq
Synthesis and biological evaluation of 1,2-disubstituted carbonucleosides of 6-substituted purine and 8-azapurine.
Nucleosides & nucleotides 1999;18(4-5):733-4.
1999: Esther Lobatón; Sonsoles Velázquez; Ana San-Félix; Cristina Chamorro; V Tuñón; A Esteban-Gamboa; Erik De Clercq; Jan Balzarini; María-José Camarasa; María-Jesús Pérez-Pérez
Novel TSAO derivatives modified at positions 3" and 4" of the spiro moiety.
Nucleosides & nucleotides 1999;18(4-5):675-6.
1999: I Nieto; María José Figueira; José Manuel Blanco; Olga Caamaño; Franco Fernández; Erik De Clercq; Jan Balzarini
Synthesis of novel carbocyclic nucleosides with a modified cyclopentane ring and evaluation of their antiviral activity.
Nucleosides & nucleotides 1999;18(4-5):641-2.
1999: JP Kleim; Mark Winters; A Dunkler; J R Suarez; G Riess; I Winkler; Jan Balzarini; D Oette; Thomas C Merigan
Antiviral activity of the human immunodeficiency virus type 1-specific nonnucleoside reverse transcriptase inhibitor HBY 097 alone and in combination with zidovudine in a phase II study. HBY 097/2001 Study Group.
The Journal of infectious diseases 1999;179(3):709-13.
1999: Sigrid Hatse; Erik De Clercq; Jan Balzarini
Impact of 9-(2-phosphonylmethoxyethyl)adenine on (deoxy)ribonucleotide metabolism and nucleic acid synthesis in tumor cells.
FEBS letters 1999;445(1):92-7.
1999: AQ Siddiqui; C Ballatore; Christopher McGuigan; Erik De Clercq; Jan Balzarini
The presence of substituents on the aryl moiety of the aryl phosphoramidate derivative of d4T enhances anti-HIV efficacy in cell culture: A structure-activity relationship.
Journal of medicinal chemistry 1999;42(3):393-9.
1999: Lieve Naesens; Sigrid Hatse; Constant Segers; Erik Verbeken; Erik De Clercq; Mark Waer; Jan Balzarini
9-(2-phosphonylmethoxyethyl)-N6-cyclopropyl-2,6-diaminopurine: a novel prodrug of 9-(2-phosphonylmethoxyethyl)guanine with improved antitumor efficacy and selectivity in choriocarcinoma-bearing rats.
Oncology research 1999;11(4):195-203.
1998: H Pelemans; Robert M Esnouf; H Jonckheere; Erik De Clercq; Jan Balzarini
Mutational analysis of Tyr-318 within the non-nucleoside reverse transcriptase inhibitor binding pocket of human immunodeficiency virus type I reverse transcriptase.
The Journal of biological chemistry 1998;273(51):34234-9.
1998: Alain Gueiffier; Sylvie Mavel; M Lhassani; A Elhakmaoui; Robert Snoeck; Graciela Andrei; Olivier Chavignon; Jean-Claude Teulade; Myriam Witvrouw; Jan Balzarini; Erik De Clercq; Jean-Pierre Chapat
Synthesis of imidazo[1,2-a]pyridines as antiviral agents.
Journal of medicinal chemistry 1998;41(25):5108-12.
1998: B Degrève; M Johansson; Erik De Clercq; Anna Karlsson; Jan Balzarini
Differential intracellular compartmentalization of herpetic thymidine kinases (TKs) in TK gene-transfected tumor cells: molecular characterization of the nuclear localization signal of herpes simplex virus type 1 TK.
Journal of virology 1998;72(12):9535-43.
1998: Sonsoles Velázquez; Cristina Chamorro; María-Jesús Pérez-Pérez; R Alvarez; María-Luisa Jimeno; A Martín-Domenech; C Pérez; Federico Gago; Erik De Clercq; Jan Balzarini; Ana San-Félix; María-José Camarasa
Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase.
Journal of medicinal chemistry 1998;41(23):4636-47.
1998: Christopher McGuigan; D Cahard; C Ballatore; Adam Siddiqui; Erik De Clercq; Jan Balzarini
Lactate cannot substitute for alanine in d4T-based anti-HIV nucleotide prodrugs--despite efficient esterase-mediated hydrolysis.
Bioorganic & medicinal chemistry letters 1998;8(21):2949-54.
1998: Sonsoles Velázquez; R Alvarez; Concepción Pérez; Federico Gago; Erik De Clercq; Jan Balzarini; María-José Camarasa
Regiospecific synthesis and anti-human immunodeficiency virus activity of novel 5-substituted N-alkylcarbamoyl and N,N-dialkylcarbamoyl 1,2,3-triazole-TSAO analogues.
Antiviral chemistry & chemotherapy 1998;9(6):481-9.
1998: Christopher McGuigan; P W Sutton; D Cahard; K Turner; G O'Leary; Y Wang; Mark Gumbleton; Erik De Clercq; Jan Balzarini
Synthesis, anti-human immunodeficiency virus activity and esterase lability of some novel carboxylic ester-modified phosphoramidate derivatives of stavudine (d4T).
Antiviral chemistry & chemotherapy 1998;9(6):473-9.
1998: Guy Van den Mooter; G Stas; Festo Damian; Lieve Naesens; Jan Balzarini; Renaat Kinget; Patrick Augustijns
Stability of UC-781, in intestinal mucosal homogenates of the rat, rabbit, and pig.
Pharmaceutical research 1998;15(11):1799-802.
1998: Sigrid Hatse; Erik De Clercq; Jan Balzarini
Enhanced 9-(2-phosphonylmethoxyethyl)adenine secretion by a specific, indomethacin-sensitive efflux pump in a mutant 9-(2-phosphonylmethoxyethyl)adenine-resistant human erythroleukemia K562 cell line.
Molecular pharmacology 1998;54(5):907-17.
1998: Jan Balzarini; A E Gamboa; Robert M Esnouf; Sandra Liekens; Johan Neyts; Erik De Clercq; María-José Camarasa; María-Jesús Pérez-Pérez
7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
FEBS letters 1998;438(1-2):91-5.
1998: E Arranz; JA Díaz; ST Ingate; Myriam Witvrouw; Christophe Pannecouque; Jan Balzarini; Erik De Clercq; S Vega
Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication.
Journal of medicinal chemistry 1998;41(21):4109-17.
1998: Jonathan R Dimmock; Sarvesh C Vashishtha; J Wilson Quail; U Pugazhenthi; Zbigniew Zimpel; Athena Sudom; Theresa M Allen; GY Kao; Jan Balzarini; Erik De Clercq
4-(beta-Arylvinyl)-3-(beta-arylvinylketo)-1-ethyl-4-piperidinols and related compounds: a novel class of cytotoxic and anticancer agents.
Journal of medicinal chemistry 1998;41(21):4012-20.
1998: Sigrid Hatse; Lieve Naesens; Erik De Clercq; Jan Balzarini
Potent differentiation-inducing properties of the antiretroviral agent 9-(2-phosphonylmethoxyethyl) adenine (PMEA) in the rat choriocarcinoma (RCHO) tumor cell model.
Biochemical pharmacology 1998;56(7):851-9.
1998: Morris J Robins; Stanislaw F Wnuk; X Yang; CS Yuan; Ronald T Borchardt; Jan Balzarini; Erik De Clercq
Inactivation of S-adenosyl-L-homocysteine hydrolase and antiviral activity with 5',5',6',6'-tetradehydro-6'-deoxy-6'-halohomoadenosine analogues (4'-haloacetylene analogues derived from adenosine).
Journal of medicinal chemistry 1998;41(20):3857-64.
1998: Cristina Chamorro; María-José Camarasa; María-Jesús Pérez-Pérez; Erik De Clercq; Jan Balzarini; Ana San-Félix
An approach towards the synthesis of potential metal-chelating TSAO-T derivatives as bidentate inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
Antiviral chemistry & chemotherapy 1998;9(5):413-22.
1998: Myriam Witvrouw; Dirk Daelemans; Christophe Pannecouque; Johan Neyts; Graciela Andrei; Robert Snoeck; Anne-Mieke Vandamme; Jan Balzarini; Jan Desmyter; M Baba; Erik De Clercq
Broad-spectrum antiviral activity and mechanism of antiviral action of the fluoroquinolone derivative K-12.
Antiviral chemistry & chemotherapy 1998;9(5):403-11.
1998: Stanislaw F Wnuk; Y Mao; CS Yuan; Ronald T Borchardt; Graciela Andrei; Jan Balzarini; Erik De Clercq; Morris J Robins
Discovery of type II (covalent) inactivation of S-adenosyl-L-homocysteine hydrolase involving its "hydrolytic activity": synthesis and evaluation of dihalohomovinyl nucleoside analogues derived from adenosine.
Journal of medicinal chemistry 1998;41(16):3078-83.
1998: Jan Balzarini; Lieve Naesens; E Verbeken; Marie Laga; Lut Van Damme; Michael A Parniak; Lieve Van Mellaert; J Anné; Erik De Clercq
Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent.
AIDS (London, England) 1998;12(10):1129-38.
1998: R Alvarez; María-Luisa Jimeno; Federico Gago; Jan Balzarini; María-Jesús Pérez-Pérez; María-José Camarasa
Novel 3'-spiro nucleoside analogues of TSAO-T. Part II. A comparative study based on NMR conformational analysis in solution and theoretical calculations.
Antiviral chemistry & chemotherapy 1998;9(4):333-40.
1998: M Isabel Nieto; José Manuel Blanco; Olga Caamaño; Franco Fernández; Xerardo García-Mera; Jan Balzarini; E Padalko; J Neyts; Erik De Clercq
Synthesis, antiviral and cytostatic activities of carbocyclic nucleosides incorporating a modified cyclopentane ring. Part 2: Adenosine and uridine analogues.
Nucleosides & nucleotides 1998;17(7):1255-66.
1998: J E Borges; Franco Fernández; X García; Antonio Rodríguez Hergueta; Carmen López; G Andrei; R Snoeck; M Witvrounw; Jan Balzarini; Erik De Clercq
Novel carbocyclic nucleosides containing a cyclobutyl ring. Guanosine and adenosine analogues.
Nucleosides & nucleotides 1998;17(7):1237-53.
1998: Lourdes Santana; Marta Teijeira; Eugenio Uriarte; Jan Balzarini; Erik De Clercq
Synthesis and biological evaluation of 1,2-disubstituted carbonucleosides of 2-amino-6-substituted purine and 8-azapurine.
Bioorganic & medicinal chemistry letters 1998;8(11):1349-52.
1998: H Pelemans; Robert M Esnouf; Michael A Parniak; Anne-Mieke Vandamme; Erik De Clercq; Jan Balzarini
A proline-to-histidine substitution at position 225 of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) sensitizes HIV-1 RT to BHAP U-90152.
The Journal of general virology 1998;79 ( Pt 6)():1347-52.
1998: A O Goldring; Jan Balzarini; Ian H Gilbert
Design and synthesis of bio-isosteres of thymidine triphosphate.
Bioorganic & medicinal chemistry letters 1998;8(10):1211-4.
1998: Sigrid Hatse; Lieve Naesens; B Degrève; Constant Segers; Michel Vandeputte; Mark Waer; Erik De Clercq; Jan Balzarini
Potent antitumor activity of the acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl)adenine in choriocarcinoma-bearing rats.
International journal of cancer. Journal international du cancer 1998;76(4):595-600.
1998: C Ochoa; R Provencio; María-Luisa Jimeno; Jan Balzarini; Erik De Clercq
Synthesis and anti-HIV properties of 1,2,4,6-thiatriazin-3-one 1,1-dioxide nucleosides.
Nucleosides & nucleotides 1998;17(5):901-10.
1998: Jan Balzarini; D Cahard; O Wedgwood; A Salgado; Sonsoles Velázquez; CJ Yarnold; Erik De Clercq; Christopher McGuigan; Halldor Thormar
Marked inhibitory activity of masked aryloxy aminoacyl phosphoramidate derivatives of dideoxynucleoside analogues against visna virus infection.
Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association 1998;17(4):296-302.
1998: Jonathan R Dimmock; NM Kandepu; M Hetherington; J Wilson Quail; U Pugazhenthi; Athena Sudom; Mahmood Chamankhah; P Rose; E Pass; Theresa M Allen; S Halleran; J Szydlowski; Bulent Mutus; M Tannous; Elias K Manavathu; Timothy G Myers; Erik De Clercq; Jan Balzarini
Cytotoxic activities of Mannich bases of chalcones and related compounds.
Journal of medicinal chemistry 1998;41(7):1014-26.
1998: Jan Balzarini; Sigrid Hatse; Lieve Naesens; Erik De Clercq
Selection and characterisation of murine leukaemia L1210 cells with high-level resistance to the cytostatic activity of the acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl) adenine (PMEA).
Biochimica et biophysica acta 1998;1402(1):29-38.
1998: Christopher McGuigan; H W Tsang; P W Sutton; Erik De Clercq; Jan Balzarini
Synthesis and anti-HIV activity of some novel chain-extended phosphoramidate derivatives of d4T (stavudine): esterase hydrolysis as a rapid predictive test for antiviral potency.
Antiviral chemistry & chemotherapy 1998;9(2):109-15.
1998: Jan Balzarini; B Degrève; Graciela Andrei; Johan Neyts; ML Sandvold; F Myhren; Erik De Clercq
Superior cytostatic activity of the ganciclovir elaidic acid ester due to the prolonged intracellular retention of ganciclovir anabolites in herpes simplex virus type 1 thymidine kinase gene-transfected tumor cells.
Gene therapy 1998;5(3):419-26.
1998: Myriam Witvrouw; M E Arranz; Christophe Pannecouque; Ruben Declercq; H Jonckheere; Jean-Claude Schmit; Anne-Mieke Vandamme; J A Diaz; ST Ingate; Jan Desmyter; Robert M Esnouf; Luc Van Meervelt; S Vega; Jan Balzarini; Erik De Clercq
1,1,3-Trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine (TTD) derivatives: a new class of nonnucleoside human immunodeficiency virus type 1 (HIV-1) reverse transcriptase inhibitors with anti-HIV-1 activity.
Antimicrobial agents and chemotherapy 1998;42(3):618-23.
1998: Jan Balzarini; H Pelemans; G Riess; M Roesner; I Winkler; Erik De Clercq; JP Kleim
Retention of marked sensitivity to (S)-4-isopropoxycarbonyl-6-methoxy-3-(methylthiomethyl)-3,4-di hydroquin oxaline-2(1H)-thione (HBY 097) by an azidothymidine (AZT)-resistant human immunodeficiency virus type 1 (HIV-1) strain subcultured in the combined presence of quinoxaline HBY 097 and 2',3'-dideoxy-3'-thiacytidine (lamivudine).
Biochemical pharmacology 1998;55(5):617-25.
1998: Jan Balzarini; H Pelemans; Robert M Esnouf; Erik De Clercq
A novel mutation (F227L) arises in the reverse transcriptase of human immunodeficiency virus type 1 on dose-escalating treatment of HIV type 1-infected cell cultures with the nonnucleoside reverse transcriptase inhibitor thiocarboxanilide UC-781.
AIDS research and human retroviruses 1998;14(3):255-60.
1998: Katrin Hartmann; M Kuffer; Jan Balzarini; Lieve Naesens; M Goldberg; Volker Erfle; Frank-Detlef Goebel; Erik De Clercq; J Jindrich; Antonin Holy; N Bischofberger; Wilfried Kraft
Efficacy of the acyclic nucleoside phosphonates (S)-9-(3-fluoro-2-phosphonylmethoxypropyl)adenine (FPMPA) and 9-(2-phosphonylmethoxyethyl)adenine (PMEA) against feline immunodeficiency virus.
Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association 1998;17(2):120-8.
1998: Lieve Naesens; D Cahard; A Salgado; L Bidois; Erik De Clercq; Christopher McGuigan; Jan Balzarini
Metabolism and anti-HIV activity of phosphoramidate derivatives of D4T-MP with variations in the amino acid moiety.
Advances in experimental medicine and biology 1998;431():753-7.
1998: Jan Balzarini; L Stet; A Matsuda; L Wiebe; E Knauss; Erik De Clercq
Metabolism of EICAR (5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide), a potent inhibitor of inosinate dehydrogenase.
Advances in experimental medicine and biology 1998;431():723-8.
1998: Sigrid Hatse; Lieve Naesens; B Degrève; Michel Vandeputte; Mark Waer; Erik De Clercq; Jan Balzarini
In vitro and in vivo inhibitory activity of the differentiation-inducing agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA) against rat choriocarcinoma.
Advances in experimental medicine and biology 1998;431():605-9.
1998: Johan Neyts; Jan Balzarini; Graciela Andrei; Z Chaoyong; Robert Snoeck; A Zimmermann; T Mertens; Anna Karlsson; Erik De Clercq
Intracellular metabolism of the N7-substituted acyclic nucleoside analog 2-amino-7-(1,3-dihydroxy-2-propoxymethyl)purine, a potent inhibitor of herpesvirus replication.
Molecular pharmacology 1998;53(1):157-65.
1997: Stefano Manfredini; Daniele Simoni; R Ferroni; R Bazzanini; Silvia Vertuani; S Hatse; Jan Balzarini; Erik De Clercq
Retinoic acid conjugates as potential antitumor agents: synthesis and biological activity of conjugates with Ara-A, Ara-C, 3(2H)-furanone, and aniline mustard moieties.
Journal of medicinal chemistry 1997;40(23):3851-7.
1997: M Kuffer; Jan Balzarini; B Rolinski; Frank-Detlef Goebel; Volker Erfle; M Goldberg; Katrin Hartmann
[Comparative investigation of the efficacy of two nucleocapsid analogs in FIV infected cats].
Tierärztliche Praxis. Ausgabe K, Kleintiere/Heimtiere 1997;25(6):671-7.
1997: Jan Balzarini; H Pelemans; G Riess; M Roesner; I Winkler; Erik De Clercq; JP Kleim
Zidovudine-resistant human immunodeficiency virus type 1 strains subcultured in the presence of both lamivudine and quinoxaline HBY 097 retain marked sensitivity to HBY 097 but not to lamivudine.
The Journal of infectious diseases 1997;176(5):1392-7.
1997: H Pelemans; Robert M Esnouf; A Dunkler; Michael A Parniak; Anne-Mieke Vandamme; Anna Karlsson; Erik De Clercq; JP Kleim; Jan Balzarini
Characteristics of the Pro225His mutation in human immunodeficiency virus type 1 (HIV-1) reverse transcriptase that appears under selective pressure of dose-escalating quinoxaline treatment of HIV-1.
Journal of virology 1997;71(11):8195-203.
1997: B Degrève; Graciela Andrei; M Izquierdo; Jacques Piette; K Morin; E E Knaus; Leonard I Wiebe; I Basrah; R T Walker; Erik De Clercq; Jan Balzarini
Varicella-zoster virus thymidine kinase gene and antiherpetic pyrimidine nucleoside analogues in a combined gene/chemotherapy treatment for cancer.
Gene therapy 1997;4(10):1107-14.
1997: K De Groote; Lieve Naesens; Jan Balzarini; Myriam Baes; Peter E Declercq
Effects of 2',3'-dideoxycytidine and 2',3'-dideoxycytidine 5'-triphosphate on phospholipid metabolism in permeabilized rat hepatocytes.
Biochemical pharmacology 1997;54(6):713-9.
1997: C Balo; Franco Fernández; E Lens; Carmen López; G Andrei; R Snoeck; Jan Balzarini; Erik De Clercq
Novel carbocyclic nucleosides containing a cyclopentyl ring. Adenosine and uridine analogues.
Archiv der Pharmazie 1997;330(8):265-7.
1997: Christopher McGuigan; H W Tsang; D Cahard; K Turner; S Velazquez; A Salgado; L Bidois; Lieve Naesens; Erik De Clercq; Jan Balzarini
Phosphoramidate derivatives of d4T as inhibitors of HIV: the effect of amino acid variation.
Antiviral research 1997;35(3):195-204.
1997: Stefano Aquaro; Carlo Federico Perno; Emanuela Balestra; Jan Balzarini; Alessandra Cenci; Mauro Francesconi; S Panti; F Serra; N Villani; Raffaele Caliò
Inhibition of replication of HIV in primary monocyte/macrophages by different antiviral drugs and comparative efficacy in lymphocytes.
Journal of leukocyte biology 1997;62(1):138-43.
1997: Jan Balzarini; J Kruining; O Wedgwood; Christophe Pannecouque; Stefano Aquaro; Carlo Federico Perno; Lieve Naesens; Myriam Witvrouw; Rudolf Heijtink; Erik De Clercq; Christopher McGuigan
Conversion of 2',3'-dideoxyadenosine (ddA) and 2',3'-didehydro-2',3'-dideoxyadenosine (d4A) to their corresponding aryloxyphosphoramidate derivatives markedly potentiates their activity against human immunodeficiency virus and hepatitis B virus.
FEBS letters 1997;410(2-3):324-8.
1997: Stanislaw F Wnuk; CS Yuan; Ronald T Borchardt; Jan Balzarini; Erik De Clercq; Morris J Robins
Anticancer and antiviral effects and inactivation of S-adenosyl-L-homocysteine hydrolase with 5'-carboxaldehydes and oximes synthesized from adenosine and sugar-modified analogues.
Journal of medicinal chemistry 1997;40(11):1608-18.
1997: Robert M Esnouf; D I Stuart; Erik De Clercq; E Schwartz; Jan Balzarini
Models which explain the inhibition of reverse transcriptase by HIV-1-specific (thio)carboxanilide derivatives.
Biochemical and biophysical research communications 1997;234(2):458-64.
1997: Jan Balzarini; Erik De Clercq; K Uberla
SIV/HIV-1 hybrid virus expressing the reverse transcriptase gene of HIV-1 remains sensitive to HIV-1-specific reverse transcriptase inhibitors after passage in rhesus macaques.
Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association 1997;15(1):1-4.
1997: Jonathan R Dimmock; Praveen Kumar; Theresa M Allen; GY Kao; S Halleran; Jan Balzarini; Erik De Clercq
Synthesis and cytotoxic evaluation of some carbohydrazones and thiocarbohydrazones of various unsaturated ketones and related Mannich bases.
Die Pharmazie 1997;52(3):182-6.
1997: Jan Balzarini; T Vahlenkamp; Herman Egberink; K Hartmann; Myriam Witvrouw; Christophe Pannecouque; P Casara; J F Navé; Erik De Clercq
Antiretroviral activities of acyclic nucleoside phosphonates [9-(2-phosphonylmethoxyethyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, (R)-9-(2-phosphonylmethoxypropyl)adenine, and MDL 74,968] in cell cultures and murine sarcoma virus-infected newborn NMRI mice.
Antimicrobial agents and chemotherapy 1997;41(3):611-6.
1997: Carlo Federico Perno; N Santoro; Emanuela Balestra; Stefano Aquaro; Alessandra Cenci; Giuseppe Lazzarino; Donato Di Pierro; Barbara Tavazzi; Jan Balzarini; Enrico Garaci; Settimio Grimaldi; Raffaele Caliò
Red blood cells mediated delivery of 9-(2-phosphonylmethoxyethyl)adenine to primary macrophages: efficiency metabolism and activity against human immunodeficiency virus or herpes simplex virus.
Antiviral research 1997;33(3):153-64.
1997: Myriam Witvrouw; Jan Balzarini; Christophe Pannecouque; S Jhaumeer-Laulloo; José A Esté; Dominique Schols; Peter Cherepanov; Jean-Claude Schmit; zeger debyser; Anne-Mieke Vandamme; Jan Desmyter; S R Ramadas; Erik De Clercq
SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus.
Antimicrobial agents and chemotherapy 1997;41(2):262-8.
1997: Jan Balzarini; H Pelemans; Erik De Clercq; Anna Karlsson; JP Kleim
Reverse transcriptase fidelity and HIV-1 variation.
Science (New York, N.Y.) 1997;275(5297):229-30; author reply 230-1.
1996: Jan Balzarini; H Pelemans; Anna Karlsson; E De ClercQ; JP Kleim
Concomitant combination therapy for HIV infection preferable over sequential therapy with 3TC and non-nucleoside reverse transcriptase inhibitors.
Proceedings of the National Academy of Sciences of the United States of America 1996;93(23):13152-7.
1996: S Ingate; E De Clercq; Jan Balzarini; María-José Camarasa
Novel L-lyxo and 5'-deoxy-5'-modified TSAO-T analogs: synthesis and anti-HIV-1 activity.
Antiviral research 1996;32(3):149-64.
1996: Sigrid Hatse; E De Clercq; Jan Balzarini
Evidence for distinction of the differentiation-inducing activities and cytostatic properties of 9-(2-phosphonylmethoxyethyl)adenine and a variety of differentiation-inducing agents in human erythroleukemia K562 cells.
Molecular pharmacology 1996;50(5):1231-42.
1996: Jan Balzarini; H Egberink; K Hartmann; D Cahard; T Vahlenkamp; H Thormar; E De Clercq; Christopher McGuigan
Antiretrovirus specificity and intracellular metabolism of 2',3' -didehydro-2',3'-dideoxythymidine (stavudine) and its 5'-monophosphate triester prodrug So324.
Molecular pharmacology 1996;50(5):1207-13.
1996: Jean-Claude Schmit; J Cogniaux; P Hermans; Christophe Van Vaeck; S Sprecher; B Van Remoortel; Myriam Witvrouw; Jan Balzarini; Jan Desmyter; E De Clercq; Anne-Mieke Vandamme
Multiple drug resistance to nucleoside analogues and nonnucleoside reverse transcriptase inhibitors in an efficiently replicating human immunodeficiency virus type 1 patient strain.
The Journal of infectious diseases 1996;174(5):962-8.
1996: Antonín Holý; H Dvoráková; J Jindrich; M Masojídková; M Budĕsínský; Jan Balzarini; G Andrei; E De Clercq
Acyclic nucleotide analogs derived from 8-azapurines: synthesis and antiviral activity.
Journal of medicinal chemistry 1996;39(20):4073-88.
1996: T Obara; S Shuto; Y Saito; R Snoeck; G Andrei; Jan Balzarini; E De Clercq; Akira Matsuda
New neplanocin analogues. 7. Synthesis and antiviral activity of 2-halo derivatives of neplanocin A.
Journal of medicinal chemistry 1996;39(19):3847-52.
1996: H Jonckheere; K De Vreese; zeger debyser; J Vandekerckhove; Jan Balzarini; Jan Desmyter; E De Clercq; Jozef Anne
A two plasmid co-expression system in Escherichia coli for the production of virion-like reverse transcriptase of the human immunodeficiency virus type 1.
Journal of virological methods 1996;61(1-2):113-25.
1996: A Tsotinis; T Calogeropoulou; M Koufaki; C Souli; Jan Balzarini; E De Clercq; Alexandros Makriyannis
Synthesis and antiretroviral evaluation of new alkoxy and aryloxy phosphate derivatives of 3'-azido-3'-deoxythymidine.
Journal of medicinal chemistry 1996;39(17):3418-22.
1996: N Kolocouris; Antonios Kolocouris; G B Foscolos; G Fytas; J Neyts; E Padalko; Jan Balzarini; R Snoeck; G Andrei; E De Clercq
Synthesis and antiviral activity evaluation of some new aminoadamantane derivatives. 2.
Journal of medicinal chemistry 1996;39(17):3307-18.
1996: H Dvoráková; M Masojídková; Antonín Holý; Jan Balzarini; G Andrei; R Snoeck; E De Clercq
Synthesis of 2'-aminomethyl derivatives of N-(2-(phosphonomethoxy)ethyl) nucleotide analogues as potential antiviral agents.
Journal of medicinal chemistry 1996;39(17):3263-8.
1996: Jan Balzarini; O Wedgwood; J Kruining; H Pelemans; R Heijtink; E De Clercq; Christopher McGuigan
Anti-HIV and anti-HBV activity and resistance profile of 2',3'-dideoxy-3'-thiacytidine (3TC) and its arylphosphoramidate derivative CF 1109.
Biochemical and biophysical research communications 1996;225(2):363-9.
1996: Jan Balzarini; H Pelemans; Stefano Aquaro; Carlo Federico Perno; Myriam Witvrouw; Dominique Schols; E De Clercq; Anna Karlsson
Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication.
Molecular pharmacology 1996;50(2):394-401.
1996: Carlo Federico Perno; Emanuela Balestra; Stefano Aquaro; S Panti; Alessandra Cenci; Giuseppe Lazzarino; Barbara Tavazzi; Donato Di Pierro; Jan Balzarini; R Calio
Potent inhibition of human immunodeficiency virus and herpes simplex virus type 1 by 9-(2-phosphonylmethoxyethyl)adenine in primary macrophages is determined by drug metabolism, nucleotide pools, and cytokines.
Molecular pharmacology 1996;50(2):359-66.
1996: Jan Balzarini; Anna Karlsson; Stefano Aquaro; Carlo Federico Perno; D Cahard; Lieve Naesens; E De Clercq; Christopher McGuigan
Mechanism of anti-HIV action of masked alaninyl d4T-MP derivatives.
Proceedings of the National Academy of Sciences of the United States of America 1996;93(14):7295-9.
1996: Els J M Van Damme; Annick Barre; P Rougé; Fred Van Leuven; Jan Balzarini; Willy J Peumans
Molecular cloning of the lectin and a lectin-related protein from common Solomon's seal (Polygonatum multiflorum).
Plant molecular biology 1996;31(3):657-72.
1996: Jan Balzarini; W G Brouwer; D C Dao; E M Osika; E De Clercq
Identification of novel thiocarboxanilide derivatives that suppress a variety of drug-resistant mutant human immunodeficiency virus type 1 strains at a potency similar to that for wild-type virus.
Antimicrobial agents and chemotherapy 1996;40(6):1454-66.
1996: Jan Balzarini; H Pelemans; María-Jesús Pérez-Pérez; Ana San-Félix; María-José Camarasa; E De Clercq; Anna Karlsson
Marked inhibitory activity of non-nucleoside reverse transcriptase inhibitors against human immunodeficiency virus type 1 when combined with (-)2',3'-dideoxy-3'-thiacytidine.
Molecular pharmacology 1996;49(5):882-90.
1996: Christopher McGuigan; D Cahard; H M Sheeka; E De Clercq; Jan Balzarini
Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite.
Journal of medicinal chemistry 1996;39(8):1748-53.
1996: Jan Balzarini; Stefano Aquaro; Carlo Federico Perno; Myriam Witvrouw; Antonín Holý; E De Clercq
Activity of the (R)-enantiomers of 9-(2-phosphonylmethoxypropyl)-adenine and 9-(2-phosphonylmethoxypropyl)-2,6-diaminopurine against human immunodeficiency virus in different human cell systems.
Biochemical and biophysical research communications 1996;219(2):337-41.
1996: Jan Balzarini; E De Clercq
Analysis of inhibition of retroviral reverse transcriptase.
Methods in enzymology 1996;275():472-502.
1996: Lieve Naesens; Jan Balzarini; Norbert Bischofberger; E De Clercq
Antiretroviral activity and pharmacokinetics in mice of oral bis(pivaloyloxymethyl)-9-(2-phosphonylmethoxyethyl)adenine, the bis(pivaloyloxymethyl) ester prodrug of 9-(2-phosphonylmethoxyethyl)adenine.
Antimicrobial agents and chemotherapy 1996;40(1):22-8.
1995: D Reymen; Lieve Naesens; Jan Balzarini; Antonín Holý; H Dvoráková; E De Clercq
Antiviral activity of selected acyclic nucleoside analogues against human herpesvirus 6.
Antiviral research 1995;28(4):343-57.
1995: Jan Balzarini; Graciela Andrei; R Kumar; E E Knaus; L I Wiebe; E De Clercq
The cytostatic activity of 5-(1-azidovinyl)-2'-deoxyuridine (AzVDU) against herpes simplex virus thymidine kinase gene-transfected FM3A cells is due to inhibition of thymidylate synthase and enhanced by UV light (lambda = 254 nm) exposure.
FEBS letters 1995;373(1):41-4.
1995: Jan Balzarini; K W Morin; E E Knaus; L I Wiebe; E De Clercq
Novel (E)-5-(2-iodovinyl)-2'-deoxyuridine derivatives as potential cytostatic agents against herpes simplex virus thymidine kinase gene transfected tumors.
Gene therapy 1995;2(5):317-22.
1995: Jan Balzarini; M Weeger; María-José Camarasa; E De Clercq; K Uberla
Sensitivity/resistance profile of a simian immunodeficiency virus containing the reverse transcriptase gene of human immunodeficiency virus type 1 (HIV-1) toward the HIV-1-specific non-nucleoside reverse transcriptase inhibitors.
Biochemical and biophysical research communications 1995;211(3):850-6.
1995: Jan Balzarini; María-Jesús Pérez-Pérez; S Vélazquez; Ana San-Félix; María-José Camarasa; E De Clercq; Anna Karlsson
Suppression of the breakthrough of human immunodeficiency virus type 1 (HIV-1) in cell culture by thiocarboxanilide derivatives when used individually or in combination with other HIV-1-specific inhibitors (i.e., TSAO derivatives).
Proceedings of the National Academy of Sciences of the United States of America 1995;92(12):5470-4.
1995: S Ingate; María-Jesús Pérez-Pérez; E De Clercq; Jan Balzarini; María-José Camarasa
Synthesis and anti-HIV-1 activity of novel TSAO-T derivatives modified at the 2'- and 5'-positions of the sugar moiety.
Antiviral research 1995;27(3):281-99.
1995: Jan Balzarini; W G Brouwer; E E Felauer; E De Clercq; Anna Karlsson
Activity of various thiocarboxanilide derivatives against wild-type and several mutant human immunodeficiency virus type 1 strains.
Antiviral research 1995;27(3):219-36.
1995: Sonsoles Velázquez; R Alvarez; Ana San-Félix; María-Luisa Jimeno; E De Clercq; Jan Balzarini; María-José Camarasa
Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase.
Journal of medicinal chemistry 1995;38(10):1641-9.
1995: Halldor Thormar; Jan Balzarini; zeger debyser; Myriam Witvrouw; Jan Desmyter; E De Clercq
Inhibition of visna virus replication and cytopathic effect in sheep choroid plexus cell cultures by selected anti-HIV agents.
Antiviral research 1995;27(1-2):49-57.
1995: Halldor Thormar; Gudmundur Georgsson; P A Pálsson; Jan Balzarini; L Naesens; Sigurbjörg Torsteinsdóttir; E De Clercq
Inhibitory effect of 9-(2-phosphonylmethoxyethyl)adenine on visna virus infection in lambs: a model for in vivo testing of candidate anti-human immunodeficiency virus drugs.
Proceedings of the National Academy of Sciences of the United States of America 1995;92(8):3283-7.
1995: Jan Balzarini; M Baba; E De Clercq
Differential activities of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives against different human immunodeficiency virus type 1 mutant strains.
Antimicrobial agents and chemotherapy 1995;39(4):998-1002.
1995: Jan Balzarini; Annemieke Verstuyf; Sigrid Hatse; Jozef Goebels; H Sobis; Michel Vandeputte; E De Clercq
The human immunodeficiency virus(HIV) inhibitor 9-(2-phosphonylmethoxyethyl)adenine (PMEA) is a strong inducer of differentiation of several tumor cell lines.
International journal of cancer. Journal international du cancer 1995;61(1):130-7.
1995: I Verheggen; Arthur Van Aerschot; Luc Van Meervelt; Jef Rozenski; L Wiebe; Robert Snoeck; Graciela Andrei; Jan Balzarini; P Claes; E De Clercq
Synthesis, biological evaluation, and structure analysis of a series of new 1,5-anhydrohexitol nucleosides.
Journal of medicinal chemistry 1995;38(5):826-35.
1995: Stefano Manfredini; Pier Giovanni Baraldi; R Bazzanini; M Marangoni; Daniele Simoni; Jan Balzarini; E De Clercq
Synthesis and cytotoxic activity of 6-vinyl- and 6-ethynyluridine and 8-vinyl-and 8-ethynyladenosine.
Journal of medicinal chemistry 1995;38(1):199-203.
1995: Lieve Naesens; Jan Balzarini; E De Clercq
The potential of acyclic nucleoside phosphonates as broad-spectrum antiviral agents.
Postepy biochemii 1995;41(5 Suppl):347-51.
1995: Jan Balzarini
Novel concepts in the treatment of human immunodeficiency virus type 1 (HIV-1) infections by HIV-1-specific reverse transcriptase inhibitors.
Verhandelingen - Koninklijke Academie voor Geneeskunde van België 1995;57(6):575-600.
1994: Johan Neyts; Graciela Andrei; Robert Snoeck; G Jähne; I Winkler; M Helsberg; Jan Balzarini; E De Clercq
The N-7-substituted acyclic nucleoside analog 2-amino-7-[(1,3-dihydroxy-2-propoxy)methyl]purine is a potent and selective inhibitor of herpesvirus replication.
Antimicrobial agents and chemotherapy 1994;38(12):2710-6.
1994: Jan Balzarini; Anna Karlsson; C Meichsner; Arnold Paessens; G Riess; E De Clercq; JP Kleim
Resistance pattern of human immunodeficiency virus type 1 reverse transcriptase to quinoxaline S-2720.
Journal of virology 1994;68(12):7986-92.
1994: R Alvarez; Sonsoles Velázquez; Ana San-Félix; Stefano Aquaro; E De Clercq; Carlo Federico Perno; Anna Karlsson; Jan Balzarini; María-José Camarasa
1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.
Journal of medicinal chemistry 1994;37(24):4185-94.
1994: Stanislaw F Wnuk; CS Yuan; R T Borchardt; Jan Balzarini; E De Clercq; Morris J Robins
Nucleic acid related compounds. 84. Synthesis of 6'-(E and Z)-halohomovinyl derivatives of adenosine, inactivation of S-adenosyl-L-homocysteine hydrolase, and correlation of anticancer and antiviral potencies with enzyme inhibition.
Journal of medicinal chemistry 1994;37(21):3579-87.
1994: H Jonckheere; J M Taymans; Jan Balzarini; Sonsoles Velázquez; María-José Camarasa; Jan Desmyter; E De Clercq; Jozef Anne
Resistance of HIV-1 reverse transcriptase against [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2''-dioxide)] (TSAO) derivatives is determined by the mutation Glu138-->Lys on the p51 subunit.
The Journal of biological chemistry 1994;269(41):25255-8.
1994: N Villani; Raffaele Caliò; Emanuela Balestra; Jan Balzarini; E De Clercq; E Fabrizi; Carlo Federico Perno; V Del Gobbo
9-(2-Phosphonylmethoxyethyl) adenine increases the survival of influenza virus-infected mice by an enhancement of the immune system.
Antiviral research 1994;25(2):81-9.
1994: Els J M Van Damme; Jan Balzarini; K Smeets; Fred Van Leuven; Willy J Peumans
The monomeric and dimeric mannose-binding proteins from the Orchidaceae species Listera ovata and Epipactis helleborine: sequence homologies and differences in biological activities.
Glycoconjugate journal 1994;11(4):321-32.
1994: Stefano Manfredini; Pier Giovanni Baraldi; R Bazzanini; M Guarneri; Daniele Simoni; Jan Balzarini; E De Clercq
Geiparvarin analogues. 4. Synthesis and cytostatic activity of geiparvarin analogues bearing a carbamate moiety or a furocoumarin fragment on the alkenyl side chain.
Journal of medicinal chemistry 1994;37(15):2401-5.
1994: Jan Balzarini; Anna Karlsson; Vinod Sardana; Emilio A Emini; María-José Camarasa; E De Clercq
Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant (E138K)RT HIV-1 mutants or select for highly resistant (Y181C-->C181I)RT HIV-1 mutants.
Proceedings of the National Academy of Sciences of the United States of America 1994;91(14):6599-603.
1994: Jan Balzarini; JP Kleim; G Riess; María-José Camarasa; E De Clercq; Anna Karlsson
Sensitivity of (138 Glu-->Lys) mutated human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) to HIV-1-specific RT inhibitors.
Biochemical and biophysical research communications 1994;201(3):1305-12.
1994: Jan Balzarini; C Bohman; R T Walker; E de Clercq
Comparative cytostatic activity of different antiherpetic drugs against herpes simplex virus thymidine kinase gene-transfected tumor cells.
Molecular pharmacology 1994;45(6):1253-8.
1994: Jan Balzarini
Metabolism and mechanism of antiretroviral action of purine and pyrimidine derivatives.
Pharmacy world & science : PWS 1994;16(2):113-26.
1994: Robert Snoeck; M Gérard; Catherine Sadzot; Graciela Andrei; Jan Balzarini; D Reymen; N Ahadi; J M De Bruyn; Jacques Piette; Bernard Rentier
Meningoradiculoneuritis due to acyclovir-resistant varicella zoster virus in an acquired immune deficiency syndrome patient.
Journal of medical virology 1994;42(4):338-47.
1994: Robert Snoeck; Graciela Andrei; M Gérard; A Silverman; A Hedderman; Jan Balzarini; Catherine Sadzot; G Tricot; N Clumeck; E De Clercq
Successful treatment of progressive mucocutaneous infection due to acyclovir- and foscarnet-resistant herpes simplex virus with (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC).
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America 1994;18(4):570-8.
1994: E De Clercq; N Yamamoto; Rudi Pauwels; Jan Balzarini; Myriam Witvrouw; K De Vreese; zeger debyser; B Rosenwirth; Peter Peichl; R Datema
Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100.
Antimicrobial agents and chemotherapy 1994;38(4):668-74.
1994: C Bohman; Jan Balzarini; piet wigerinck; Arthur Van Aerschot; Piet Herdewijn; E De Clercq
Mechanism of cytostatic action of novel 5-(thien-2-yl)- and 5-(furan-2-yl)-substituted pyrimidine nucleoside analogues against tumor cells transfected by the thymidine kinase gene of herpes simplex virus.
The Journal of biological chemistry 1994;269(11):8036-43.
1994: Ana San-Félix; Sonsoles Velázquez; María-Jesús Pérez-Pérez; Jan Balzarini; E De Clercq; María-José Camarasa
Novel series of TSAO-T derivatives. Synthesis and anti-HIV-1 activity of 4-, 5-, and 6-substituted pyrimidine analogues.
Journal of medicinal chemistry 1994;37(4):453-60.
1994: Raffaele Caliò; N Villani; Emanuela Balestra; F Sesa; A Holy; Jan Balzarini; E De Clercq; Carlo Federico Perno; V Del Gobbo
Enhancement of natural killer activity and interferon induction by different acyclic nucleoside phosphonates.
Antiviral research 1994;23(1):77-89.
1993: Halldor Thormar; Jan Balzarini; A Holy; J Jindrich; I Rosenberg; zeger debyser; Jan Desmyter; E De Clercq
Inhibition of visna virus replication by 2',3'-dideoxynucleosides and acyclic nucleoside phosphonate analogs.
Antimicrobial agents and chemotherapy 1993;37(12):2540-4.
1993: Jan Balzarini; A Karlsson; L Wang; C Bohman; K Horská; Ivan Votruba; A Fridland; Arthur Van Aerschot; Piet Herdewijn; E De Clercq
Eicar (5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide). A novel potent inhibitor of inosinate dehydrogenase activity and guanylate biosynthesis.
The Journal of biological chemistry 1993;268(33):24591-8.
1993: Robert Snoeck; M Gérard; Catherine Sadzot; Graciela Andrei; Jan Balzarini; D Reymen; Jacques Piette; Bernard Rentier; N Clumeck; E De Clercq
Meningoradiculoneuritis due to acyclovir-resistant varicella-zoster virus in a patient with AIDS.
The Journal of infectious diseases 1993;168(5):1330-1.
1993: Sonsoles Velázquez; Ana San-Félix; María-Jesús Pérez-Pérez; Jan Balzarini; E De Clercq; María-José Camarasa
TSAO analogues. 3. Synthesis and anti-HIV-1 activity of 2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl 3'-spiro-5''-(4''-amino-1'',2''-oxathiole 2'',2''-dioxide) purine and purine-modified nucleosides.
Journal of medicinal chemistry 1993;36(22):3230-9.
1993: Els J M Van Damme; K Smeets; I Engelborghs; H Aelbers; Jan Balzarini; A Pusztai; Fred Van Leuven; Irwin J Goldstein; Willy J Peumans
Cloning and characterization of the lectin cDNA clones from onion, shallot and leek.
Plant molecular biology 1993;23(2):365-76.
1993: María-Jesús Pérez-Pérez; Jan Balzarini; E De Clercq; María-José Camarasa
Glycosyl-oxycarbonylaminosulfonyl-2',3'-dideoxynucleoside derivatives as lipophilic nucleotide mimics. Synthesis and anti-HIV activity.
Bioorganic & medicinal chemistry 1993;1(4):279-84.
1993: Jan Balzarini; Anna Karlsson; E De Clercq
Human immunodeficiency virus type 1 drug-resistance patterns with different 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives.
Molecular pharmacology 1993;44(4):694-701.
1993: Jan Balzarini; Anna Karlsson; María-Jesús Pérez-Pérez; María-José Camarasa; E De Clercq
Knocking-out concentrations of HIV-1-specific inhibitors completely suppress HIV-1 infection and prevent the emergence of drug-resistant virus.
Virology 1993;196(2):576-85.
1993: Jan Balzarini; Anna Karlsson; María-Jesús Pérez-Pérez; María-José Camarasa; W G Tarpley; E De Clercq
Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combinations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy.
Journal of virology 1993;67(9):5353-9.
1993: A Papadaki-Valiraki; Spyroula Papakonstantinou-Garoufalias; P Marakos; A Chytyroglou-Lada; M Hosoya; Jan Balzarini; E de Clercq
Synthesis, antifungal, antibacterial and antiviral effects of some adamantaneketoxime ethers.
Farmaco (Società chimica italiana : 1989) 1993;48(8):1091-102.
1993: Jan Balzarini; Anna Karlsson; Anne-Mieke Vandamme; María-Jesús Pérez-Pérez; Hong Zhang; Lotta Vrang; B Oberg; Kristina Bäckbro; Torsten Unge; Ana San-Félix
Human immunodeficiency virus type 1 (HIV-1) strains selected for resistance against the HIV-1-specific [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro- 5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)]-beta-D-pentofurano syl (TSAO) nucleoside analogues retain sensitivity to HIV-1-specific nonnucleoside inhibitors.
Proceedings of the National Academy of Sciences of the United States of America 1993;90(15):6952-6.
1993: I Verheggen; Arthur Van Aerschot; S Toppet; Robert Snoeck; G Janssen; Jan Balzarini; E De Clercq; Piet Herdewijn
Synthesis and antiherpes virus activity of 1,5-anhydrohexitol nucleosides.
Journal of medicinal chemistry 1993;36(14):2033-40.
1993: Jan Balzarini; Lieve Naesens; C Bohman; María-Jesús Pérez-Pérez; Ana San-Félix; María-José Camarasa; E De Clercq
Metabolism and pharmacokinetics of the anti-HIV-1-specific inhibitor [1-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3-N- methyl-thymine]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dio xide).
Biochemical pharmacology 1993;46(1):69-77.
1993: Robert Snoeck; Graciela Andrei; Johan Neyts; Dominique Schols; M Cools; Jan Balzarini; E De Clercq
Inhibitory activity of S-adenosylhomocysteine hydrolase inhibitors against human cytomegalovirus replication.
Antiviral research 1993;21(3):197-216.
1993: Christopher McGuigan; R N Pathirana; Jan Balzarini; E De Clercq
Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT.
Journal of medicinal chemistry 1993;36(8):1048-52.
1993: Jan Balzarini; C Bohman; E De Clercq
Differential mechanism of cytostatic effect of (E)-5-(2-bromovinyl)-2'-deoxyuridine, 9-(1,3-dihydroxy-2-propoxymethyl)guanine, and other antiherpetic drugs on tumor cells transfected by the thymidine kinase gene of herpes simplex virus type 1 or type 2.
The Journal of biological chemistry 1993;268(9):6332-7.
1993: Jan Balzarini; A Holy; J Jindrich; Lieve Naesens; Robert Snoeck; Dominique Schols; E De Clercq
Differential antiherpesvirus and antiretrovirus effects of the (S) and (R) enantiomers of acyclic nucleoside phosphonates: potent and selective in vitro and in vivo antiretrovirus activities of (R)-9-(2-phosphonomethoxypropyl)-2,6-diaminopurine.
Antimicrobial agents and chemotherapy 1993;37(2):332-8.
1993: Lieve Naesens; Johan Neyts; Jan Balzarini; A Holy; I Rosenberg; E De Clercq
Efficacy of oral 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) in the treatment of retrovirus and cytomegalovirus infections in mice.
Journal of medical virology 1993;39(2):167-72.
1993: Jan Balzarini; Anna Karlsson; María-Jesús Pérez-Pérez; Lotta Vrang; J Walbers; Hong Zhang; B Oberg; Anne-Mieke Vandamme; María-José Camarasa; E De Clercq
HIV-1-specific reverse transcriptase inhibitors show differential activity against HIV-1 mutant strains containing different amino acid substitutions in the reverse transcriptase.
Virology 1993;192(1):246-53.
1993: Jan Balzarini; S Velazquez; ANA SAN-FELIX; Anna Karlsson; M J Perez-Perez; María-José Camarasa; E De Clercq
Human immunodeficiency virus type 1-specific [2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodeficiency virus type 1-specific non-nucleoside analogues.
Molecular pharmacology 1993;43(1):109-14.
1992: Robert Snoeck; Graciela Andrei; Dominique Schols; Jan Balzarini; E De Clercq
Activity of different antiviral drug combinations against human cytomegalovirus replication in vitro.
European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology 1992;11(12):1144-55.
1992: N Yamamoto; Dominique Schols; E De Clercq; zeger debyser; Rudi Pauwels; Jan Balzarini; H Nakashima; M Baba; M Hosoya; Robert Snoeck
Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents.
Molecular pharmacology 1992;42(6):1109-17.
1992: Jan Balzarini; E De Clercq
Assay method for monitoring the inhibitory effects of antimetabolites on the activity of inosinate dehydrogenase in intact human CEM lymphocytes.
The Biochemical journal 1992;287 ( Pt 3)():785-90.
1992: Lieve Naesens; Jan Balzarini; E De Clercq
Pharmacokinetics in mice of the anti-retrovirus agent 9-(2-phosphonylmethoxyethyl)adenine.
Drug metabolism and disposition: the biological fate of chemicals 1992;20(5):747-52.
1992: Alberto Bergamini; Carlo Federico Perno; Jan Balzarini; Marcella Capozzi; L Marinelli; G Milanese; C D Pesce; R Calió; Giovanni Rocchi
Selective inhibition of HIV replication by adriamycin in macrophages but not in lymphocytes.
AIDS research and human retroviruses 1992;8(7):1239-47.
1992: Johan Neyts; Robert Snoeck; Dominique Schols; Jan Balzarini; J D Esko; Ann Van Schepdael; E De Clercq
Sulfated polymers inhibit the interaction of human cytomegalovirus with cell surface heparan sulfate.
Virology 1992;189(1):48-58.
1992: E De Clercq; N Yamamoto; Rudi Pauwels; M Baba; Dominique Schols; H Nakashima; Jan Balzarini; zeger debyser; B A Murrer; D Schwartz
Potent and selective inhibition of human immunodeficiency virus (HIV)-1 and HIV-2 replication by a class of bicyclams interacting with a viral uncoating event.
Proceedings of the National Academy of Sciences of the United States of America 1992;89(12):5286-90.
1992: Jan Balzarini; María-Jesús Pérez-Pérez; Ana San-Félix; María-José Camarasa; I C Bathurst; P J Barr; E De Clercq
Kinetics of inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase by the novel HIV-1-specific nucleoside analogue [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5 "- (4"-amino-1",2"-oxathiole-2",2"-dioxide)thymine (TSAO-T).
The Journal of biological chemistry 1992;267(17):11831-8.
1992: Morris J Robins; V Samano; W Zhang; Jan Balzarini; E De Clercq; R T Borchardt; Y Lee; CS Yuan
Nucleic acid related compounds. 74. Synthesis and biological activity of 2'(and 3')-deoxy-2'(and 3')-methylenenucleoside analogues that function as mechanism-based inhibitors of S-adenosyl-L-homocysteine hydrolase and/or ribonucleotide reductase.
Journal of medicinal chemistry 1992;35(12):2283-93.
1992: Jan Balzarini; Johan Neyts; Dominique Schols; M Hosoya; Els J M Van Damme; Willy J Peumans; E De Clercq
The mannose-specific plant lectins from Cymbidium hybrid and Epipactis helleborine and the (N-acetylglucosamine)n-specific plant lectin from Urtica dioica are potent and selective inhibitors of human immunodeficiency virus and cytomegalovirus replication in vitro.
Antiviral research 1992;18(2):191-207.
1992: Pier Giovanni Baraldi; Stefano Manfredini; Daniele Simoni; M A Tabrizi; Jan Balzarini; E De Clercq
Geiparvarin analogues. 3. Synthesis and cytostatic activity of 3(2H)-furanone and 4,5-dihydro-3(2H)-furanone congeners of geiparvarin, containing a geraniol-like fragment in the side chain.
Journal of medicinal chemistry 1992;35(10):1877-82.
1992: Jan Balzarini; María-Jesús Pérez-Pérez; Ana San-Félix; Dominique Schols; Carlo Federico Perno; Anne-Mieke Vandamme; María-José Camarasa; E De Clercq
2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2'-dioxide)pyrimidine (TSAO) nucleoside analogues: highlyselective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase.
Proceedings of the National Academy of Sciences of the United States of America 1992;89(10):4392-6.
1992: Jan Balzarini; María-Jesús Pérez-Pérez; Ana San-Félix; S Velazquez; María-José Camarasa; E De Clercq
[2',5'-Bis-O-(tert-butyldimethylsilyl)]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide) (TSAO) derivatives of purine and pyrimidinenucleosides as potent and selective inhibitors of human immunodeficiency virus type 1.
Antimicrobial agents and chemotherapy 1992;36(5):1073-80.
1992: Lieve Naesens; Jan Balzarini; E De Clercq
Acyclic adenine nucleoside phosphonates in plasma determined by high-performance liquid chromatography with fluorescence detection.
Clinical chemistry 1992;38(4):480-5.
1992: Carlo Federico Perno; R Yarchoan; Jan Balzarini; Alberto Bergamini; G Milanese; R Pauwels; E De Clercq; Giovanni Rocchi; R Calio
Different pattern of activity of inhibitors of the human immunodeficiency virus in lymphocytes and monocyte/macrophages.
Antiviral research 1992;17(4):289-304.
1992: S Shuto; T Obara; M Toriya; M Hosoya; R Snoeck; G Andrei; Jan Balzarini; E De Clercq
New neplanocin analogues. 1. Synthesis of 6'-modified neplanocin A derivatives as broad-spectrum antiviral agents.
Journal of medicinal chemistry 1992;35(2):324-31.
1991: M Hosoya; Jan Balzarini; S Shigeta; E De Clercq
Differential inhibitory effects of sulfated polysaccharides and polymers on the replication of various myxoviruses and retroviruses, depending on the composition of the target amino acid sequences of the viral envelope glycoproteins.
Antimicrobial agents and chemotherapy 1991;35(12):2515-20.
1991: Jan Balzarini; C K Lee; Piet Herdewijn; E De Clercq
Mechanism of the potentiating effect of ribavirin on the activity of 2',3'-dideoxyinosine against human immunodeficiency virus.
The Journal of biological chemistry 1991;266(32):21509-14.
1991: Daniele Simoni; Stefano Manfredini; M A Tabrizi; R Bazzanini; Pier Giovanni Baraldi; Jan Balzarini; E De Clercq
Geiparvarin analogues. 2. Synthesis and cytostatic activity of 5-(4-arylbutadienyl)-3(2H)-furanones and of N-substituted 3-(4-oxo-2-furanyl)-2-buten-2-yl carbamates.
Journal of medicinal chemistry 1991;34(11):3172-6.
1991: Jan Balzarini; C K Lee; Dominique Schols; E De Clercq
1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamide (ribavirin) and 5-ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) markedly potentiate the inhibitory effect of 2',3'-dideoxyinosine on human immunodeficiency virus in peripheral blood lymphocytes.
Biochemical and biophysical research communications 1991;178(2):563-9.
1991: Jan Balzarini; Carlo Federico Perno; Dominique Schols; E De Clercq
Activity of acyclic nucleoside phosphonate analogues against human immunodeficiency virus in monocyte/macrophages and peripheral blood lymphocytes.
Biochemical and biophysical research communications 1991;178(1):329-35.
1991: Lieve Naesens; Jan Balzarini; E De Clercq
Single-dose administration of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) and 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP) in the prophylaxis of retrovirus infection in vivo.
Antiviral research 1991;16(1):53-64.
1991: V Del Gobbo; A Foli; Jan Balzarini; E De Clercq; Emanuela Balestra; N Villani; S Marini; Carlo Federico Perno; R Calio
Immunomodulatory activity of 9-(2-phosphonylmethoxyethyl)adenine (PMEA), a potent anti-HIV nucleotide analogue, on in vivo murine models.
Antiviral research 1991;16(1):65-75.
1991: Johan Neyts; Robert Snoeck; Jan Balzarini; E De Clercq
Particular characteristics of the anti-human cytomegalovirus activity of (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine (HPMPC) in vitro.
Antiviral research 1991;16(1):41-52.
1991: M Cools; Jan Balzarini; E De Clercq
Mechanism of antiviral and cytotoxic action of (+/-)-6' beta-fluoroaristeromycin, a potent inhibitor of S-adenosylhomocysteine hydrolase.
Molecular pharmacology 1991;39(6):718-24.
1991: Jan Balzarini; A Holy; J Jindrich; H Dvorakova; Z Hao; Robert Snoeck; Piet Herdewijn; D G Johns; E De Clercq
9-[(2RS)-3-fluoro-2-phosphonylmethoxypropyl] derivatives of purines: a class of highly selective antiretroviral agents in vitro and in vivo.
Proceedings of the National Academy of Sciences of the United States of America 1991;88(11):4961-5.
1991: Jan Balzarini; E De Clercq
5-Phosphoribosyl 1-pyrophosphate synthetase converts the acyclic nucleoside phosphonates 9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine and 9-(2-phosphonylmethoxyethyl)adenine directly to their antivirally active diphosphate derivatives.
The Journal of biological chemistry 1991;266(14):8686-9.
1991: E De Clercq; M Cools; Jan Balzarini; Robert Snoeck; Graciela Andrei; M Hosoya; S Shigeta; T Ueda; N Minakawa; A Matsuda
Antiviral activities of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4- carboxamide and related compounds.
Antimicrobial agents and chemotherapy 1991;35(4):679-84.
1991: Jan Balzarini; Dominique Schols; Johan Neyts; Els J M Van Damme; Willy J Peumans; E De Clercq
Alpha-(1-3)- and alpha-(1-6)-D-mannose-specific plant lectins are markedly inhibitory to human immunodeficiency virus and cytomegalovirus infections in vitro.
Antimicrobial agents and chemotherapy 1991;35(3):410-6.
1991: Jan Balzarini; Z Hao; Piet Herdewijn; D G Johns; E De Clercq
Intracellular metabolism and mechanism of anti-retrovirus action of 9-(2-phosphonylmethoxyethyl)adenine, a potent anti-human immunodeficiency virus compound.
Proceedings of the National Academy of Sciences of the United States of America 1991;88(4):1499-503.
1991: Jan Balzarini; Lieve Naesens; J Slachmuylders; H Niphuis; I Rosenberg; Antonín Holý; H Schellekens; E De Clercq
9-(2-Phosphonylmethoxyethyl)adenine (PMEA) effectively inhibits retrovirus replication in vitro and simian immunodeficiency virus infection in rhesus monkeys.
AIDS (London, England) 1991;5(1):21-8.
1991: Jan Balzarini; E De Clercq
Conversion of acyclic nucleoside phosphonates to their diphosphate derivatives by 5-phosphoribosyl-1-pyrophosphate (PRPP) synthetase.
Advances in experimental medicine and biology 1991;309A():29-32.
1990: Jan Balzarini; E De Clercq
9-Beta-D-arabinofuranosyladenine 5'-monophosphate (araAMP) is converted directly to its antivirally active 5'-triphosphate form by 5-phosphoribosyl-1-pyrophosphate (PRPP) synthetase.
Biochemical and biophysical research communications 1990;173(3):781-7.
1990: Arthur Van Aerschot; D Everaert; G Gosselin; Oswald M Peeters; Norbert Blaton; Camiel J De Ranter; J L Imbach; Jan Balzarini; E De Clercq; Piet Herdewijn
2'-Azido-2',3'-dideoxythymidine: synthesis and crystal structure of a 2'-substituted dideoxynucleoside.
Antiviral research 1990;14(6):357-69.
1990: Johan Neyts; Robert Snoeck; Dominique Schols; Jan Balzarini; E De Clercq
Selective inhibition of human cytomegalovirus DNA synthesis by (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine [(S)-HPMPC] and 9-(1,3-dihydroxy-2-propoxymethyl)guanine (DHPG).
Virology 1990;179(1):41-50.
1990: L Jie; Arthur Van Aerschot; Jan Balzarini; G Janssen; Roger Busson; Jos Hoogmartens; E De Clercq; Piet Herdewijn
5'-O-phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity.
Journal of medicinal chemistry 1990;33(9):2481-7.
1990: Jan Balzarini; Lieve Naesens; E De Clercq
Anti-retrovirus activity of 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in vivo increases when it is less frequently administered.
International journal of cancer. Journal international du cancer 1990;46(2):337-40.
1990: Robert Snoeck; Laurence Lagneaux; Alain Delforge; Dominique Bron; P Van der Auwera; P Stryckmans; Jan Balzarini; E De Clercq
Inhibitory effects of potent inhibitors of human immunodeficiency virus and cytomegalovirus on the growth of human granulocyte-macrophage progenitor cells in vitro.
European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology 1990;9(8):615-9.
1990: H Nakashima; Jan Balzarini; Rudi Pauwels; Dominique Schols; Jan Desmyter; E De Clercq
Anti-HIV-1 activity of antiviral compounds, as quantitated by a focal immunoassay in CD4+ HeLa cells and a plaque assay in MT-4 cells.
Journal of virological methods 1990;29(2):197-208.
1990: Arthur Van Aerschot; D Everaert; Jan Balzarini; Koen Augustyns; L Jie; G Janssen; Oswald M Peeters; Norbert Blaton; Camiel J De Ranter; E De Clercq
Synthesis and anti-HIV evaluation of 2',3'-dideoxyribo-5-chloropyrimidine analogues: reduced toxicity of 5-chlorinated 2',3'-dideoxynucleosides.
Journal of medicinal chemistry 1990;33(6):1833-9.
1990: Jan Balzarini; H Sobis; Lieve Naesens; Michel Vandeputte; E De Clercq
Inhibitory effects of 9-(2-phosphonylmethoxyethyl)adenine and 3'-azido-2',3'-dideoxythymidine on tumor development in mice inoculated intracerebrally with Moloney murine sarcoma virus.
International journal of cancer. Journal international du cancer 1990;45(3):486-9.
1990: Jan Balzarini; R Bernaerts; A Verbruggen; E De Clercq
Role of the incorporation of (E)-5-(2-iodovinyl)-2'-deoxyuridine and its carbocyclic analogue into DNA of herpes simplex virus type 1-infected cells in the antiviral effects of these compounds.
Molecular pharmacology 1990;37(3):402-7.
1990: Jan Balzarini; E De Clercq; H Baumgartner; M Bodenteich; Herfried Griengl
Carbocyclic 5-iodo-2'-deoxyuridine (C-IDU) and carbocyclic (E)-5-(2-bromovinyl)-2'-deoxyuridine (C-BVDU) as unique examples of chiral molecules where the two enantiomeric forms are biologically active: interaction of the (+)- and (-)-enantiomers of C-IDU and C-BVDU with the thymidine kinase of herpes simplex virus type 1.
Molecular pharmacology 1990;37(3):395-401.
1990: piet wigerinck; Arthur Van Aerschot; G Janssen; P Claes; Jan Balzarini; E De Clercq; Piet Herdewijn
Synthesis and antiviral activity of 3'-heterocyclic substituted 3'-deoxythymidines.
Journal of medicinal chemistry 1990;33(2):868-73.
1990: Jan Balzarini; Lieve Naesens; M J Robins; E De Clercq
Potentiating effect of ribavirin on the in vitro and in vivo antiretrovirus activities of 2',3'-dideoxyinosine and 2',3'-dideoxy-2,6-diaminopurine riboside.
Journal of acquired immune deficiency syndromes 1990;3(12):1140-7.
1990: Myriam Witvrouw; M Baba; Jan Balzarini; Rudi Pauwels; E De Clercq
Establishment of a bioassay to determine serum levels of dextran sulfate and pentosan polysulfate, two potent inhibitors of human immunodeficiency virus.
Journal of acquired immune deficiency syndromes 1990;3(4):343-7.
1989: M Baba; H Tanaka; E De Clercq; Rudi Pauwels; Jan Balzarini; Dominique Schols; H Nakashima; Carlo Federico Perno; R T Walker; T Miyasaka
Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative.
Biochemical and biophysical research communications 1989;165(3):1375-81.
1989: Lieve Naesens; Jan Balzarini; I Rosenberg; Antonín Holý; E De Clercq
9-(2-Phosphonylmethoxyethyl)-2,6-diaminopurine (PMEDAP): a novel agent with anti-human immunodeficiency virus activity in vitro and potent anti-Moloney murine sarcoma virus activity in vivo.
European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology 1989;8(12):1043-7.
1989: Jan Balzarini; Arthur Van Aerschot; Piet Herdewijn; E De Clercq
2',3'-didehydro-2',3'-dideoxy-5-chlorocytidine is a selective anti-retrovirus agent.
Biochemical and biophysical research communications 1989;164(3):1190-7.
1989: Morris J Robins; S G Wood; N K Dalley; Piet Herdewijn; Jan Balzarini; E De Clercq
Nucleic acid related compounds. 57. Synthesis, x-ray crystal structure, lipophilic partition properties, and antiretroviral activities of anomeric 3'-azido-2',3'-dideoxy-2,6-diaminopurine ribosides.
Journal of medicinal chemistry 1989;32(8):1763-8.
1989: Arthur Van Aerschot; Piet Herdewijn; Jan Balzarini; Rudi Pauwels; E De Clercq
3'-Fluoro-2',3'-dideoxy-5-chlorouridine: most selective anti-HIV-1 agent among a series of new 2'- and 3'-fluorinated 2',3'-dideoxynucleoside analogues.
Journal of medicinal chemistry 1989;32(8):1743-9.
1989: E De Clercq; M Cools; Jan Balzarini; V E Marquez; D R Borcherding; R T Borchardt; J C Drach; S Kitaoka; T Konno
Broad-spectrum antiviral activities of neplanocin A, 3-deazaneplanocin A, and their 5'-nor derivatives.
Antimicrobial agents and chemotherapy 1989;33(8):1291-7.
1989: Jan Balzarini; H Baumgartner; M Bodenteich; E De Clercq; Herfried Griengl
Synthesis and antiviral activity of the enantiomeric forms of carba-5-iodo-2'-deoxyuridine and carba-(E)-5-(2-bromovinyl)-2'-deoxyuridine.
Journal of medicinal chemistry 1989;32(8):1861-5.
1989: E De Clercq; M Cools; Jan Balzarini
Homocysteine potentiates the antiviral and cytostatic activity of those nucleoside analogues that are targeted at S-adenosylhomocysteine hydrolase.
Biochemical pharmacology 1989;38(11):1771-8.
1989: Jan Balzarini; E De Clercq
Inhibitory effects of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) and related compounds on herpes simplex virus (HSV)-infected cells and HSV thymidine kinase gene-transformed cells.
Methods and findings in experimental and clinical pharmacology 1989;11(6):379-89.
1989: Jan Balzarini; Arthur Van Aerschot; Rudi Pauwels; M Baba; Dominique Schols; Piet Herdewijn; E De Clercq
5-Halogeno-3'-fluoro-2',3'-dideoxyuridines as inhibitors of human immunodeficiency virus (HIV): potent and selective anti-HIV activity of 3'-fluoro-2',3'-dideoxy-5-chlorouridine.
Molecular pharmacology 1989;35(5):571-7.
1989: Jan Balzarini; Piet Herdewijn; E De Clercq
Potentiating effect of ribavirin on the anti-retrovirus activity of 3'-azido-2,6-diaminopurine-2',3'-dideoxyriboside in vitro and in vivo.
Antiviral research 1989;11(4):161-71.
1989: Jan Balzarini; Piet Herdewijn; E De Clercq
Differential patterns of intracellular metabolism of 2',3'-didehydro-2',3'-dideoxythymidine and 3'-azido-2',3'-dideoxythymidine, two potent anti-human immunodeficiency virus compounds.
The Journal of biological chemistry 1989;264(11):6127-33.
1989: Jan Balzarini; Arthur Van Aerschot; Piet Herdewijn; E de Clercq
5-Chloro-substituted derivatives of 2', 3'-didehydro-2',3'-dideoxyuridine, 3'-fluoro-2',3'-dideoxyuridine and 3'-azido-2',3'-dideoxyuridine as anti-HIV agents.
Biochemical pharmacology 1989;38(6):869-74.
1989: Jan Balzarini; E De Clercq
The antiviral activity of 9-beta-D-arabinofuranosyladenine is enhanced by the 2',3'-dideoxyriboside, the 2',3'-didehydro-2',3'-dideoxyriboside and the 3'-azido-2',3'-dideoxyriboside of 2,6-diaminopurine.
Biochemical and biophysical research communications 1989;159(1):61-7.
1989: Pier Giovanni Baraldi; M Guarneri; Stefano Manfredini; Daniele Simoni; Jan Balzarini; E De Clercq
Synthesis and cytostatic activity of geiparvarin analogues.
Journal of medicinal chemistry 1989;32(2):284-8.
1989: Jan Balzarini; M Cools; E De Clercq
Estimation of the lipophilicity of anti-HIV nucleoside analogues by determination of the partition coefficient and retention time on a Lichrospher 60 RP-8 HPLC column.
Biochemical and biophysical research communications 1989;158(2):413-22.
1989: Jan Balzarini; Lieve Naesens; Piet Herdewijn; I Rosenberg; A Holy; Rudi Pauwels; M Baba; D G Johns; E De Clercq
Marked in vivo antiretrovirus activity of 9-(2-phosphonylmethoxyethyl)adenine, a selective anti-human immunodeficiency virus agent.
Proceedings of the National Academy of Sciences of the United States of America 1989;86(1):332-6.
1989: Jan Balzarini; E Matthes; P Meeus; D G Johns; E De Clercq
The antiretroviral and cytostatic activity, and metabolism of 3'-azido-2',3'-dideoxythymidine, 3'-fluoro-2',3'-dideoxythymidine and 2',3'-dideoxycytidine are highly cell type-dependent.
Advances in experimental medicine and biology 1989;253B():407-13.
1988: Dominique Schols; Rudi Pauwels; F Vanlangendonck; Jan Balzarini; E De Clercq
A highly reliable, sensitive, flow cytometric/fluorometric assay for the evaluation of the anti-HIV activity of antiviral compounds in MT-4 cells.
Journal of immunological methods 1988;114(1-2):27-32.
1988: Piet Herdewijn; Jan Balzarini; M Baba; Rudi Pauwels; Arthur Van Aerschot; G Janssen; E De Clercq
Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides.
Journal of medicinal chemistry 1988;31(10):2040-8.
1988: M Baba; Dominique Schols; Rudi Pauwels; Jan Balzarini; E De Clercq
Fuchsin acid selectively inhibits human immunodeficiency virus (HIV) replication in vitro.
Biochemical and biophysical research communications 1988;155(3):1404-11.
1988: M Baba; M Nakajima; Dominique Schols; Rudi Pauwels; Jan Balzarini; E De Clercq
Pentosan polysulfate, a sulfated oligosaccharide, is a potent and selective anti-HIV agent in vitro.
Antiviral research 1988;9(6):335-43.
1988: Rudi Pauwels; Jan Balzarini; M Baba; Robert Snoeck; Dominique Schols; Piet Herdewijn; Jan Desmyter; E De Clercq
Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds.
Journal of virological methods 1988;20(4):309-21.
1988: M Baba; Rudi Pauwels; Jan Balzarini; J Arnout; Jan Desmyter; E De Clercq
Mechanism of inhibitory effect of dextran sulfate and heparin on replication of human immunodeficiency virus in vitro.
Proceedings of the National Academy of Sciences of the United States of America 1988;85(16):6132-6.
1988: Jan Balzarini; M Baba; Rudi Pauwels; Piet Herdewijn; E De Clerq
Anti-retrovirus activity of 3'-fluoro- and 3'-azido-substituted pyrimidine 2',3'-dideoxynucleoside analogues.
Biochemical pharmacology 1988;37(14):2847-56.
1988: Rudi Pauwels; Jan Balzarini; Dominique Schols; M Baba; Jan Desmyter; I Rosenberg; A Holy; E De Clercq
Phosphonylmethoxyethyl purine derivatives, a new class of anti-human immunodeficiency virus agents.
Antimicrobial agents and chemotherapy 1988;32(7):1025-30.
1988: Jan Balzarini; Piet Herdewijn; Rudi Pauwels; S Broder; E De Clercq
Alpha, beta- and beta, gamma-methylene 5'-phosphonate derivatives of 3'-azido-2',3'-dideoxythymidine-5'-triphosphate. Correlation between affinity for reverse transcriptase, susceptibility to hydrolysis by phosphodiesterases and anti-retrovirus activity.
Biochemical pharmacology 1988;37(12):2395-403.
1988: Rudi Pauwels; M Baba; Jan Balzarini; Piet Herdewijn; Jan Desmyter; M J Robins; R M Zou; D Madej; E De Clercq
Investigations on the anti-HIV activity of 2',3'-dideoxyadenosine analogues with modifications in either the pentose or purine moiety. Potent and selective anti-HIV activity of 2,6-diaminopurine 2',3'-dideoxyriboside.
Biochemical pharmacology 1988;37(7):1317-25.
1988: H J Keizer; R Pauwels; Willy Landuyt; Jan Balzarini; E van der Schueren; E De Clercq
Combined effects of bromovinyldeoxyuridine and fractionated or continuous administration of 5-fluorouracil in P388 leukemia-bearing mice.
Cancer letters 1988;39(2):217-23.
1988: Jan Balzarini; M Baba; Rudi Pauwels; Piet Herdewijn; S G Wood; M J Robins; E de Clercq