Jan Balzarini

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Jenabian Mohammad-Ali; Saïdi Héla; Charpentier Charlotte; Van Herrewege Yven; Son Jong Chan; Schols Dominique; Balzarini Jan; Vanham Guido; Bélec Laurent;
In vitro synergistic activity against CCR5-tropic HIV-1 with combinations of potential candidate microbicide molecules HHA, KRV2110 and enfuvirtide (T20).
McGuigan Christopher; Derudas Marco; Quintiliani Maurizio; Andrei Graciela; Snoeck Robert; Henson Geoffrey; Balzarini Jan
2'-Fluorosugar analogues of the highly potent anti-varicella-zoster virus bicyclic nucleoside analogue (BCNA) Cf 1743.
Youssef Dani; Potter Elizabeth; Jha Mamta; De Clercq Erik; Balzarini Jan; Stables James P; Jha Amitabh
Design, synthesis and bioevaluation of novel maleamic amino acid ester conjugates of 3,5-bisarylmethylene-4-piperidones as cytostatic agents.

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2009: Jenabian Mohammad-Ali; Saïdi Héla; Charpentier Charlotte; Van Herrewege Yven; Son Jong Chan; Schols Dominique; Balzarini Jan; Vanham Guido; Bélec Laurent;
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: McGuigan Christopher; Derudas Marco; Quintiliani Maurizio; Andrei Graciela; Snoeck Robert; Henson Geoffrey; Balzarini Jan
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: Youssef Dani; Potter Elizabeth; Jha Mamta; De Clercq Erik; Balzarini Jan; Stables James P; Jha Amitabh
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: Das Swagatika; Das Umashankar; Selvakumar Ponniah; Sharma Rajendra K; Balzarini Jan; De Clercq Erik; Molnár Joseph; Serly Julianna; Baráth Zoltán; Schatte Gabriele; Bandy Brian; Gorecki Dennis K J; Dimmock Jonathan R
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: Mehellou Youcef; Balzarini Jan; McGuigan Christopher
Aryloxy phosphoramidate triesters: a technology for delivering monophosphorylated nucleosides and sugars into cells.
ChemMedChem 2009;4(11):1779-91.
2009: François Katrien O; Pannecouque Christophe; Auwerx Joeri; Lozano Virginia; Pérez-Pérez Maria-Jésus; Schols Dominique; Balzarini Jan
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: Manta Stella; Tzioumaki Niki; Tsoukala Evangelia; Panagiotopoulou Aggeliki; Pelecanou Maria; Balzarini Jan; Komiotis Dimitri
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: Bronckaers Annelies; Gago Federico; Balzarini Jan; Liekens Sandra
The dual role of thymidine phosphorylase in cancer development and chemotherapy.
Medicinal research reviews 2009;29(6):903-53.
2009: Sharma Deepika; Narasimhan Balasubramanian; Kumar Pradeep; Judge Vikramjeet; Narang Rakesh; De Clercq Erik; Balzarini Jan
Synthesis, antimicrobial and antiviral activity of substituted benzimidazoles.
Journal of enzyme inhibition and medicinal chemistry 2009;24(5):1161-8.
2009: Romagnoli Romeo; Baraldi Pier Giovanni; Carrion Maria Dora; Cara Carlota Lopez; Cruz-Lopez Olga; Tolomeo Manlio; Grimaudo Stefania; Di Cristina Antonietta; Pipitone Maria Rosaria; Balzarini Jan; Zonta Nicola; Brancale Andrea; Hamel Ernest
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: McGuigan Christopher; Balzarini Jan
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: Auvynet Constance; Topalis Dimitri; Caillat Christophe; Munier-Lehmann Hélène; Seclaman Edward; Balzarini Jan; Agrofoglio Luigi André; Kaminski Pierre Alexandre; Meyer Philippe; Deville-Bonne Dominique; El Amri Chahrazade
Phosphorylation of dGMP analogs by vaccinia virus TMP kinase and human GMP kinase.
Biochemical and biophysical research communications 2009;388(1):6-11.
2009: Romagnoli Romeo; Baraldi Pier Giovanni; Carrion Maria Dora; Cruz-Lopez Olga; Cara Carlota Lopez; Basso Giuseppe; Viola Giampietro; Khedr Mohammed; Balzarini Jan; Mahboobi Siavosh; Sellmer Andreas; Brancale Andrea; Hamel Ernest
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: Derudas Marco; Carta Davide; Brancale Andrea; Vanpouille Christophe; Lisco Andrea; Margolis Leonid; Balzarini Jan; McGuigan Christopher
The application of phosphoramidate protide technology to acyclovir confers anti-HIV inhibition.
Journal of medicinal chemistry 2009;52(17):5520-30.
2009: Liang Yong-Hong; Feng Xiao-Qing; Zeng Zhao-Sen; Chen Fen-Er; Balzarini Jan; Pannecouque Christophe; De Clercq Erik
Design, synthesis, and SAR of naphthyl-substituted Diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
ChemMedChem 2009;4(9):1537-45.
2009: Curbo Sophie; Johansson Magnus; Balzarini Jan; Lewis Lionel D; Karlsson Anna
Acute cytotoxicity of arabinofuranosyl nucleoside analogs is not dependent on mitochondrial DNA.
Experimental cell research 2009;315(15):2539-43.
2009: el-Sabbagh Osama I; Baraka Mohamed M; Ibrahim Samy M; Pannecouque Christophe; Andrei Graciela; Snoeck Robert; Balzarini Jan; Rashad Adel A
Synthesis and antiviral activity of new pyrazole and thiazole derivatives.
European journal of medicinal chemistry 2009;44(9):3746-53.
2009: Tchesnokov Egor P; Obikhod Aleksandr; Massud Ivana; Lisco Andrea; Vanpouille Christophe; Brichacek Beda; Balzarini Jan; McGuigan Christopher; Derudas Marco; Margolis Leonid; Schinazi Raymond F; Götte Matthias
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: Bronckaers A; Aguado L; Negri A; Camarasa M-J; Balzarini J; Pérez-Pérez M-J; Gago F; Liekens S
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: Tevyashova Anna N; Olsufyeva Eugenia N; Turchin Konstantin F; Balzarini Jan; Bykov Eugenyi E; Dezhenkova Lyubov G; Shtil Alexander A; Preobrazhenskaya Maria N
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: Auwerx Joeri; François Katrien O; Vanstreels Els; Van Laethem Kristel; Daelemans Dirk; Schols Dominique; Balzarini Jan
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: Mehellou Youcef; Balzarini Jan; McGuigan Christopher
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: Liekens Sandra; Bronckaers Annelies; Balzarini Jan
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: Tzioumaki Niki; Tsoukala Evangelia; Manta Stella; Agelis George; Balzarini Jan; Komiotis Dimitri
Synthesis, antiviral and cytostatic evaluation of unsaturated exomethylene and keto D-lyxopyranonucleoside analogues.
Archiv der Pharmazie 2009;342(6):353-60.
2009: Koszytkowska-Stawinska Mariola; De Clercq Erik; Balzarini Jan
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: Gisch Nicolas; Balzarini Jan; Meier Chris
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: Das Umashankar; Pati Hari N; Panda Atulya K; De Clercq Erik; Balzarini Jan; Molnár Joseph; Baráth Zoltán; Ocsovszki Imre; Kawase Masami; Zhou Li; Sakagami Hiroshi; Dimmock Jonathan R
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: Manta Stella; Tsoukala Evangelia; Tzioumaki Niki; Goropevsek Ales; Pamulapati Ravi Teja; Cencic Avrelija; Balzarini Jan; Komiotis Dimitri
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: Liu Bo; Peng Hao; Yao Qing; Li Jing; Van Damme Els; Balzarini Jan; Bao Jin-ku
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: Auwerx Joeri; Isacsson Ola; Söderlund Johan; Balzarini Jan; Johansson Magnus; Lundberg Mathias
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: Sharma Deepika; Narasimhan Balasubramanian; Kumar Pradeep; Judge Vikramjeet; Narang Rakesh; De Clercq Erik; Balzarini Jan
Synthesis, antimicrobial and antiviral evaluation of substituted imidazole derivatives.
European journal of medicinal chemistry 2009;44(6):2347-53.
2009: Robins Morris J; Yang Hong; Miranda Karl; Peterson Matt A; De Clercq Erik; Balzarini Jan
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: Balzarini Jan; Van Daele Ineke; Negri Ana; Solaroli Nicola; Karlsson Anna; Liekens Sandra; Gago Federico; Van Calenbergh Serge
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: Xiong Yuan-Zhen; Chen Fen-Er; Balzarini Jan; De Clercq Erik; Pannecouque Christophe
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: McGuigan Christopher; Bidet Olivier; Derudas Marco; Andrei Graciela; Snoeck Robert; Balzarini Jan
Alkenyl substituted bicyclic nucleoside analogues retain nanomolar potency against Varicella Zoster Virus.
Bioorganic & medicinal chemistry 2009;17(8):3025-7.
2009: Piscitelli Francesco; Coluccia Antonio; Brancale Andrea; La Regina Giuseppe; Sansone Anna; Giordano Cesare; Balzarini Jan; Maga Giovanni; Zanoli Samantha; Samuele Alberta; Cirilli Roberto; La Torre Francesco; Lavecchia Antonio; Novellino Ettore; Silvestri Romano
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: Alen Marijke M F; Kaptein Suzanne J F; De Burghgraeve Tine; Balzarini Jan; Neyts Johan; Schols Dominique
Antiviral activity of carbohydrate-binding agents and the role of DC-SIGN in dengue virus infection.
Virology 2009;387(1):67-75.
2009: Romagnoli Romeo; Baraldi Pier Giovanni; Carrion Maria Dora; Cruz-Lopez Olga; Cara Carlota Lopez; Balzarini Jan; Hamel Ernest; Canella Alessandro; Fabbri Enrica; Gambari Roberto; Basso Giuseppe; Viola Giampietro
Hybrid alpha-bromoacryloylamido chalcones. Design, synthesis and biological evaluation.
Bioorganic & medicinal chemistry letters 2009;19(7):2022-8.
2009: Karki Subhas S; Bahaduria Vivek Singh; Rana Vivek; Kumar Sujeet; Subbaro Prasanna G; Das Umashankar; Balzarini Jan; De Clercq Erik; Dimmock Jonathan R
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: Ozturk Ibrahim I; Hadjikakou Sotiris K; Hadjiliadis Nick; Kourkoumelis Nikolaos; Kubicki Maciej; Tasiopoulos Anastasios J; Scleiman Hanadi; Barsan Mirela M; Butler Ian S; Balzarini Jan
New antimony(III) bromide complexes with thioamides: synthesis, characterization, and cytostatic properties.
Inorganic chemistry 2009;48(5):2233-45.
2009: De Castro Sonia; García-Aparicio Carlos; Andrei Graciela; Snoeck Robert; Balzarini Jan; Camarasa María-José; Velázquez Sonsoles
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: Shchekotikhin Andrey E; Glazunova Valeria A; Dezhenkova Lyubov G; Luzikov Yuri N; Sinkevich Yuri B; Kovalenko Leonid V; Buyanov Vladimir N; Balzarini Jan; Huang Fong-Chun; Lin Jing-Jer; Huang Hsu-Shan; Shtil Alexander A; Preobrazhenskaya Maria N
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: Rajic Zrinka; Butula Ivan; Zorc Branka; Kraljevic Pavelic Sandra; Hock Karlo; Pavelic Kresimir; Naesens Lieve; De Clercq Erik; Balzarini Jan; Przyborowska Monika; Ossowski Tadeusz; Mintas Mladen
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: Fouquaert Elke; Smith David F; Peumans Willy J; Proost Paul; Balzarini Jan; Savvides Savvas N; Damme Els J M Van
Related lectins from snowdrop and maize differ in their carbohydrate-binding specificity.
Biochemical and biophysical research communications 2009;380(2):260-5.
2009: Lv Hui; Kong Yang; Yao Qing; Zhang Bo; Leng Fang-Wei; Bian He-Jiao; Balzarini Jan; Van Damme Els; Bao Jin-Ku
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: Wang Yue-Ping; Chen Fen-Er; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Xiong Yuan-Zhen; Hu Hai-Rong; Chen Fen-Er; Balzarini Jan; Pannecouque Christophe; de Clercq Erik
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: Chamorro Cristina; Kruijtzer John A W; Farsaraki Marina; Balzarini Jan; Liskamp Rob M J
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: Feng Xiao-Qing; Liang Yong-Hong; Zeng Zhao-Sen; Chen Fen-Er; Balzarini Jan; Pannecouque Christophe; De Clercq Erik
Structural modifications of DAPY analogues with potent anti-HIV-1 activity.
ChemMedChem 2009;4(2):219-24.
2009: Tevyashova Anna N; Olsufyeva Eugenia N; Balzarini Jan; Shtil Alexander A; Dezhenkova Lyubov G; Bukhman Vladimir M; Zbarsky Victor B; Preobrazhenskaya Maria N
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: Wittine K; Benci K; Rajic Z; Zorc B; Kralj M; Marjanovic M; Pavelic K; De Clercq E; Andrei G; Snoeck R; Balzarini J; Mintas M
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: Pati Hari N; Das Umashankar; Das Swagatika; Bandy Brian; De Clercq Erik; Balzarini Jan; Kawase Masami; Sakagami Hiroshi; Quail J Wilson; Stables James P; Dimmock Jonathan R
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: Balzarini Jan; Orzeszko-Krzesinska Barbara; Maurin Jan K; Orzeszko Andrzej
Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones.
European journal of medicinal chemistry 2009;44(1):303-11.
2009: Haraguchi Kazuhiro; Shimada Hisashi; Akutsu Genta; Kimura Keigo; Tanaka Hiromichi; Hamasaki Takayuki; Baba Masanori; Gullen Elizabeth A; Dutschman Ginger E; Cheng Yung-Chi; Balzarini Jan
Synthesis and anti-HIV activity of 4'-C-ethynyl-2'-deoxy-4'-thio-nucleosides.
Nucleic acids symposium series (2004) 2009;(53):97-8.
2009: Meyer Philippe; Caillat Christophe; Topalis Dimitri; Balzarini Jan; Deville-Bonne Dominique
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: Kubota Yutaka; Ishizaki Nobuhide; Kaneda Yuri; Haraguchi Kazuhiro; Odanaka Yuki; Tanaka Hiromichi; Kato Nobuyuki; Baba Masanori; Balzarini Jan
Synthesis and antiviral evaluation of 4'-alkoxy analogues of 9-(beta-D-xylofuranosyl)adenine.
Antiviral chemistry & chemotherapy 2009;19(5):201-12.
2009: Abdurahman Samir; Végvári Akos; Levi Michael; Höglund Stefan; Högberg Marita; Tong Weimin; Romero Ivan; Balzarini Jan; Vahlne Anders
Isolation and characterization of a small antiretroviral molecule affecting HIV-1 capsid morphology.
Retrovirology 2009;6():34.
2008: Auwerx Joeri; François Katrien O; Covens Kris; Van Laethem Kristel; Balzarini Jan
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: Romagnoli Romeo; Baraldi Pier Giovanni; Sarkar Taradas; Cara Carlota Lopez; Lopez Olga Cruz; Carrion Maria Dora; Preti Delia; Tolomeo Manlio; Balzarini Jan; Hamel Ernest
Synthesis and biological evaluation of 2-aroyl-4-phenyl-5-hydroxybenzofurans as a new class of antitubulin agents.
Medicinal chemistry (Shariqah (United Arab Emirates)) 2008;4(6):558-64.
2008: Caillat Christophe; Topalis Dimitri; Agrofoglio Luigi A; Pochet Sylvie; Balzarini Jan; Deville-Bonne Dominique; Meyer Philippe
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: Gisch Nicolas; Balzarini Jan; Meier Chris
Studies on enzyme-cleavable dialkoxymethyl-cyclosaligenyl-2',3'-dideoxy-2',3'-didehydrothymidine monophosphates.
Journal of medicinal chemistry 2008;51(21):6752-60.
2008: Jessen Henning J; Balzarini Jan; Meier Chris
Intracellular trapping of cycloSal-pronucleotides: modification of prodrugs with amino acid esters.
Journal of medicinal chemistry 2008;51(20):6592-8.
2008: Abdurahman Samir; Végvári Akos; Youssefi Masoud; Levi Michael; Höglund Stefan; Andersson Elin; Horal Peter; Svennerholm Bo; Balzarini Jan; Vahlne Anders
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: Lisco Andrea; Vanpouille Christophe; Tchesnokov Egor P; Grivel Jean-Charles; Biancotto Angélique; Brichacek Beda; Elliott Julie; Fromentin Emilie; Shattock Robin; Anton Peter; Gorelick Robert; Balzarini Jan; McGuigan Christopher; Derudas Marco; Götte Matthias; Schinazi Raymond F; Margolis Leonid
Acyclovir is activated into a HIV-1 reverse transcriptase inhibitor in herpesvirus-infected human tissues.
Cell host & microbe 2008;4(3):260-70.
2008: Romagnoli Romeo; Baraldi Pier Giovanni; Sarkar Taradas; Carrion Maria Dora; Cruz-Lopez Olga; Lopez Cara Carlota; Tolomeo Manlio; Grimaudo Stefania; Di Cristina Antonietta; Pipitone Maria Rosaria; Balzarini Jan; Gambari Roberto; Ilaria Lampronti; Saletti Roberto; Brancale Andrea; Hamel Ernest
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: Romagnoli Romeo; Baraldi Pier Giovanni; Carrion Maria Dora; Cruz-Lopez Olga; Cara Carlota Lopez; Tolomeo Manlio; Grimaudo Stefania; Di Cristina Antonietta; Pipitone Maria Rosa; Balzarini Jan; Kandil Sahar; Brancale Andrea; Sarkar Taradas; Hamel Ernest
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: Tabarrini Oriana; Massari Serena; Daelemans Dirk; Stevens Miguel; Manfroni Giuseppe; Sabatini Stefano; Balzarini Jan; Cecchetti Violetta; Pannecouque Christophe; Fravolini Arnaldo
Structure-activity relationship study on anti-HIV 6-desfluoroquinolones.
Journal of medicinal chemistry 2008;51(17):5454-8.
2008: de Castro Sonia; Peromingo M Teresa; Naesens Lieve; Andrei Graciela; Snoeck Robert; Balzarini Jan; Velázquez Sonsoles; Camarasa María-José
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: Pérez-Pérez María-Jesús; Priego Eva-María; Hernández Ana-Isabel; Familiar Olga; Camarasa María-José; Negri Ana; Gago Federico; Balzarini Jan
Structure, physiological role, and specific inhibitors of human thymidine kinase 2 (TK2): present and future.
Medicinal research reviews 2008;28(5):797-820.
2008: McGuigan Christopher; Derudas Marco; Bugert Joachim J; Andrei Graciela; Snoeck Robert; Balzarini Jan
Successful kinase bypass with new acyclovir phosphoramidate prodrugs.
Bioorganic & medicinal chemistry letters 2008;18(15):4364-7.
2008: Balestrieri Emanuela; Ascolani Arianna; Igarashi Yasuhiro; Oki Toshikazu; Mastino Antonio; Balzarini Jan; Macchi Beatrice
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: François Katrien O; Auwerx Joeri; Schols Dominique; Balzarini Jan
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: Solaroli N; Johansson M; Persoons L; Balzarini J; Karlsson A
Substrate specificity of feline and canine herpesvirus thymidine kinase.
Antiviral research 2008;79(2):128-32.
2008: Gerland Béatrice; Désiré Jérôme; Balzarini Jan; Décout Jean-Luc
Anti-retroviral and cytostatic activity of 2',3'-dideoxyribonucleoside 3'-disulfides.
Bioorganic & medicinal chemistry 2008;16(14):6824-31.
2008: Bronckaers Annelies; Balzarini Jan; Liekens Sandra
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: Bjerke M; Balzarini J; Karlsson A
Reduced levels of mitochondrial DNA increases the toxicity of 9-beta-D-arabinofuranosylguanine (araG).
Nucleosides, nucleotides & nucleic acids 2008;27(6):746-9.
2008: Lougiakis Nikolaos; Marakos Panagiotis; Pouli Nicole; Balzarini Jan
Synthesis and antiviral activity evaluation of some novel acyclic C-nucleosides.
Chemical & pharmaceutical bulletin 2008;56(6):775-80.
2008: Das Umashankar; Doroudi Alireza; Das Swagatika; Bandy Brian; Balzarini Jan; De Clercq Erik; Dimmock Jonathan R
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: Perkovic Ivana; Butula Ivan; Zorc Branka; Hock Karlo; Kraljevic Pavelic Sandra; Pavelic Kresimir; Clercq Erik De; Balzarini Jan; Mintas Mladen
Novel lipophilic hydroxyurea derivatives: synthesis, cytostatic and antiviral activity evaluations.
Chemical biology & drug design 2008;71(6):546-53.
2008: Xiong Yuan-Zhen; Chen Fen-Er; Balzarini Jan; De Clercq Erik; Pannecouque Christophe
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: Romagnoli Romeo; Baraldi Pier Giovanni; Carrion Maria Dora; Cara Carlota Lopez; Cruz-Lopez Olga; Preti Delia; Tolomeo Manlio; Grimaudo Stefania; Di Cristina Antonella; Zonta Nicola; Balzarini Jan; Brancale Andrea; Sarkar Taradas; Hamel Ernest
Design, synthesis, and biological evaluation of thiophene analogues of chalcones.
Bioorganic & medicinal chemistry 2008;16(10):5367-76.
2008: Gazivoda Tatjana; Raic-Malic Silvana; Kristafor Vedran; Makuc Damjan; Plavec Janez; Bratulic Sinisa; Kraljevic-Pavelic Sandra; Pavelic Kresimir; Naesens Lieve; Andrei Graciela; Snoeck Robert; Balzarini Jan; Mintas Mladen
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: Pati Hari N; Das Umashankar; Kawase Masami; Sakagami Hiroshi; Balzarini Jan; De Clercq Erik; Dimmock Jonathan R
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: Bonache María-Cruz; Quesada Ernesto; Sheen Chih-Wei; Balzarini Jan; Sluis-Cremer Nicolas; Pérez-Pérez María Jesús; Camarasa María-José; San-Félix Ana
Novel N-3 substituted TSAO-T derivatives: synthesis and anti-HIV-evaluation.
Nucleosides, nucleotides & nucleic acids 2008;27(4):351-67.
2008: Tomassi Cyrille; Nguyen Van Nhien Albert; Marco-Contelles José; Balzarini Jan; Pannecouque Christophe; De Clercq Erik; Soriano Elena; Postel Denis
Synthesis, anti-HIV-1 activity, and modeling studies of N-3 Boc TSAO compound.
Bioorganic & medicinal chemistry letters 2008;18(7):2277-81.
2008: Tomassi Cyrille; Nguyen Van Nhien Albert; Marco-Contelles José; Balzarini Jan; Pannecouque Christophe; De Clercq Erik; Postel Denis
Synthesis and anti-HIV1 biological activity of novel 5''-ATSAO compounds.
Bioorganic & medicinal chemistry 2008;16(8):4733-41.
2008: Wang Yue-Ping; Chen Fen-Er; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Perjési Pal; Das Umashankar; De Clercq Erik; Balzarini Jan; Kawase Masame; Sakagami Hiroshi; Stables James P; Lorand Tamas; Rozmer Zsuzsanna; Dimmock Jonathan R
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: Romagnoli Romeo; Baraldi Pier Giovanni; Sarkar Taradas; Carrion Maria Dora; Cara Carlota Lopez; Cruz-Lopez Olga; Preti Delia; Tabrizi Mojgan Aghazadeh; Tolomeo Manlio; Grimaudo Stefania; Di Cristina Antonella; Zonta Nicola; Balzarini Jan; Brancale Andrea; Hsieh Hsing-Pang; Hamel Ernest
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: D'Onofrio Jennifer; Petraccone Luigi; Martino Luigi; Di Fabio Giovanni; Iadonisi Alfonso; Balzarini Jan; Giancola Concetta; Montesarchio Daniela
Synthesis, biophysical characterization, and anti-HIV activity of glyco-conjugated G-quadruplex-forming oligonucleotides.
Bioconjugate chemistry 2008;19(3):607-16.
2008: Bjerke Mia; Franco Maribel; Johansson Magnus; Balzarini Jan; Karlsson Anna
Increased mitochondrial DNA copy-number in CEM cells resistant to delayed toxicity of 2',3'-dideoxycytidine.
Biochemical pharmacology 2008;75(6):1313-21.
2008: Jasamai Malina; Balzarini Jan; Simons Claire
6-Azathymidine-4'-thionucleosides: synthesis and antiviral evaluation.
Journal of enzyme inhibition and medicinal chemistry 2008;23(1):56-61.
2008: Wang Yueping; Chen Fen-Er; Balzarini Jan; De Clercq Erik; Pannecouque Christophe
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.
2008: Pollicita M; Schols D; Aquaro S; Peumans W J; Van Damme E J M; Perno C F; Balzarini J
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: Jessen Henning Jacob; Schulz Tilmann; Balzarini Jan; Meier Chris
Bioreversible protection of nucleoside diphosphates.
Angewandte Chemie (International ed. in English) 2008;47(45):8719-22.
2008: Rai Diwakar; Yadav Dipti; Balzarini J; De Clercq E; Singh Ramendra K
Design and development of curcumin bioconjugates as antiviral agents.
Nucleic acids symposium series (2004) 2008;(52):599-600.
2008: Yadav Dipti; Rai Diwakar; Balzarini J; De Clercq E; Singh Ramendra K
Thymidine analogs as potential antiviral agents.
Nucleic acids symposium series (2004) 2008;(52):263-4.
2008: Meier C; Jessen H J; Balzarini J
Nucleoside diphosphate prodrugs.
Nucleic acids symposium series (2004) 2008;(52):83-4.
2008: Huskens Dana; Vermeire Kurt; Vandemeulebroucke Elise; Balzarini Jan; Schols Dominique
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.
2007: Migliore Marco D; Zonta Nicola; McGuigan Christopher; Henson Geoffrey; Andrei Graciela; Snoeck Robert; Balzarini Jan
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: Chitneni Satish K; Deroose Christophe M; Balzarini Jan; Gijsbers Rik; Celen Sofie; Debyser Zeger; Mortelmans Luc; Verbruggen Alfons M; Bormans Guy M
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: McGuigan Christopher; Pathirana Ranjith N; Migliore Marco; Adak Rina; Luoni Giovanna; Jones Arwyn T; Díez-Torrubia Alberto; Camarasa Maria-Jose; Velázquez Sonsoles; Henson Geoffrey; Verbeken Erik; Sienaert Rebecca; Naesens Lieve; Snoeck Robert; Andrei Graciela; Balzarini Jan
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: El Akri Khalid; Bougrin Khalid; Balzarini Jan; Faraj Abdesslem; Benhida Rachid
Efficient synthesis and in vitro cytostatic activity of 4-substituted triazolyl-nucleosides.
Bioorganic & medicinal chemistry letters 2007;17(23):6656-9.
2007: Solaroli Nicola; Zheng Xinyu; Johansson Magnus; Balzarini Jan; Karlsson Anna
Mitochondrial expression of the Drosophila melanogaster multisubstrate deoxyribonucleoside kinase.
Molecular pharmacology 2007;72(6):1593-8.
2007: Liekens Sandra; Bronckaers Annelies; Pérez-Pérez Maria-Jésus; Balzarini Jan
Targeting platelet-derived endothelial cell growth factor/thymidine phosphorylase for cancer therapy.
Biochemical pharmacology 2007;74(11):1555-67.
2007: Romagnoli Romeo; Baraldi Pier Giovanni; Remusat Vincent; Carrion Maria Dora; Cara Carlota Lopez; Cruz-Lopez Olga; Preti Delia; Fruttarolo Francesca; Tabrizi Mojgan Aghazadeh; Balzarini Jan; Hamel Ernest
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 (Shariqah (United Arab Emirates)) 2007;3(6):507-12.
2007: Krecmerová Marcela; Holý Antonín; Pohl Radek; Masojídková Milena; Andrei Graciela; Naesens Lieve; Neyts Johan; Balzarini Jan; De Clercq Erik; Snoeck Robert
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: Van Daele Ineke; Munier-Lehmann Hélène; Froeyen Matheus; Balzarini Jan; Van Calenbergh Serge
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: Karki Subhas S; Thota Sreekanth; Darj Satyanarayana Y; Balzarini Jan; De Clercq Erik
Synthesis, anticancer, and cytotoxic activities of some mononuclear Ru(II) compounds.
Bioorganic & medicinal chemistry 2007;15(21):6632-41.
2007: García-Aparicio Carlos; Diez-Torrubia Alberto; Balzarini Jan; Lambeir Anne-Marie; Velázquez Sonsoles; Camarasa María-José
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: Ozturk Ibrahim I; Hadjikakou Sotiris K; Hadjiliadis Nick; Kourkoumelis Nikolaos; Kubicki Maciej; Baril Martin; Butler Ian S; Balzarini Jan
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: Youssef Dani; Nichols Christie E; Cameron T Stanley; Balzarini Jan; De Clercq Erik; Jha Amitabh
Design, synthesis, and cytostatic activity of novel cyclic curcumin analogues.
Bioorganic & medicinal chemistry letters 2007;17(20):5624-9.
2007: Ceccherini-Silberstein Francesca; Svicher Valentina; Sing Tobias; Artese Anna; Santoro Maria Mercedes; Forbici Federica; Bertoli Ada; Alcaro Stefano; Palamara Guido; d'Arminio Monforte Antonella; Balzarini Jan; Antinori Andrea; Lengauer Thomas; Perno Carlo Federico
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: Troshina Olesya A; Troshin Pavel A; Peregudov Alexander S; Kozlovskiy Viacheslav I; Balzarini Jan; Lyubovskaya Rimma N
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: Jha Amitabh; Mukherjee Chandrani; Prasad Ashok K; Parmar Virinder S; Clercq Erik De; Balzarini Jan; Stables James P; Manavathu Elias K; Shrivastav Anuraag; Sharma Rajendra K; Nienaber Kurt H; Zello Gordon A; Dimmock Jonathan R
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: Bertaux Claire; Daelemans Dirk; Meertens Laurent; Cormier Emmanuel G; Reinus John F; Peumans Willy J; Van Damme Els J M; Igarashi Yasuhiro; Oki Toshikazu; Schols Dominique; Dragic Tatjana; Balzarini Jan
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: Keyaerts Els; Vijgen Leen; Pannecouque Christophe; Van Damme Els; Peumans Willy; Egberink Herman; Balzarini Jan; Van Ranst Marc
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: Gazivoda Tatjana; Sokcevic Mario; Kralj Marijeta; Suman Lidija; Pavelic Kresimir; De Clercq Erik; Andrei Graciela; Snoeck Robert; Balzarini Jan; Mintas Mladen; Raic-Malic Silvana
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: Balzarini Jan
Targeting the glycans of glycoproteins: a novel paradigm for antiviral therapy.
Nature reviews. Microbiology 2007;5(8):583-97.
2007: Robins Morris J; Nowak Ireneusz; Rajwanshi Vivek K; Miranda Karl; Cannon John F; Peterson Matt A; Andrei Graciela; Snoeck Robert; De Clercq Erik; Balzarini Jan
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: Jha Amitabh; Mukherjee Chandrani; Rolle Alfred J; De Clercq Erik; Balzarini Jan; Stables James P
Cytostatic activity of novel 4'-aminochalcone-based imides.
Bioorganic & medicinal chemistry letters 2007;17(16):4545-50.
2007: Stevens Miguel; Balzarini Jan; Lagoja Irene M; Noppen Bernard; François Katrien; Van Aerschot Arthur; Herdewijn Piet; De Clercq Erik; Pannecouque Christophe
Inhibition of human immunodeficiency virus type 1 transcription by N-aminoimidazole derivatives.
Virology 2007;365(1):220-37.
2007: Mehellou Youcef; McGuigan Christopher; Brancale Andrea; Balzarini Jan
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: Balzarini Jan; Orzeszko Barbara; Maurin Jan K; Orzeszko Andrzej
Synthesis and anti-HIV studies of 2-adamantyl-substituted thiazolidin-4-ones.
European journal of medicinal chemistry 2007;42(7):993-1003.
2007: Prekupec Svjetlana; Makuc Damjan; Plavec Janez; Suman Lidija; Kralj Marijeta; Pavelic Kresimir; Balzarini Jan; Clercq Erik De; Mintas Mladen; Raic-Malic Silvana
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: Cristofoli Walter A; Wiebe Leonard I; De Clercq Erik; Andrei Graciela; Snoeck Robert; Balzarini Jan; Knaus Edward E
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: Chitneni Satish K; Deroose Christophe M; Fonge Humphrey; Gijsbers Rik; Dyubankova Natalia; Balzarini Jan; Debyser Zeger; Mortelmans Luc; Verbruggen Alfons M; Bormans Guy M
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: Zhang Xinying; Amer Adel; Fan Xuesen; Balzarini Jan; Neyts Johan; De Clercq Erik; Prichard Mark; Kern Earl; Torrence Paul F
Synthesis and antiviral activities of new acyclic and "double-headed" nucleoside analogues.
Bioorganic chemistry 2007;35(3):221-32.
2007: Luo Yongting; Xu Xiaochao; Liu Jiwei; Li Jian; Sun Yisheng; Liu Zhen; Liu Jinzhi; Van Damme Els; Balzarini Jan; Bao Jinku
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: Balzarini Jan
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: Romagnoli Romeo; Baraldi Pier Giovanni; Carrion Maria Dora; Lopez Cara Carlota; Preti Delia; Fruttarolo Francesca; Pavani Maria Giovanna; Tabrizi Mojgan Aghazadeh; Tolomeo Manlio; Grimaudo Stefania; Di Cristina Antonella; Balzarini Jan; Hadfield John A; Brancale Andrea; Hamel Ernest
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: Huang Weiqiang; Miller Marvin J; De Clercq Erik; Balzarini Jan
Syntheses and anti-HIV activities of (+/-)-norcarbovir and (+/-)-norabacavir.
Organic & biomolecular chemistry 2007;5(8):1164-6.
2007: Celen Sofie; de Groot Tjibbe; Balzarini Jan; Vunckx Kathleen; Terwinghe Christelle; Vermaelen Peter; Van Berckelaer Lizette; Vanbilloen Hubert; Nuyts Johan; Mortelmans Luc; Verbruggen Alfons; Bormans Guy
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: Ji Lei; Chen Fen-Er; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Gisch Nicolas; Balzarini Jan; Meier Chris
Enzymatically activated cycloSal-d4T-monophosphates: The third generation of cycloSal-pronucleotides.
Journal of medicinal chemistry 2007;50(7):1658-67.
2007: Ciliberti Nunzia; Manfredini Stefano; Angusti Angela; Durini Elisa; Solaroli Nicola; Vertuani Silvia; Buzzoni Lisa; Bonache Maria Cruz; Ben-Shalom Efrat; Karlsson Anna; Saada Ann; Balzarini Jan
Novel selective human mitochondrial kinase inhibitors: design, synthesis and enzymatic activity.
Bioorganic & medicinal chemistry 2007;15(8):3065-81.
2007: Barreca Maria Letizia; Rao Angela; De Luca Laura; Iraci Nunzio; Monforte Anna-Maria; Maga Giovanni; De Clercq Erik; Pannecouque Christophe; Balzarini Jan; Chimirri Alba
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: Stevens Miguel; Pollicita Michela; Pannecouque Christophe; Verbeken Erik; Tabarrini Oriana; Cecchetti Violetta; Aquaro Stefano; Perno Carlo Federico; Fravolini Arnaldo; De Clercq Erik; Schols Dominique; Balzarini Jan
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: Huskens Dana; Van Laethem Kristel; Vermeire Kurt; Balzarini Jan; Schols Dominique
Resistance of HIV-1 to the broadly HIV-1-neutralizing, anti-carbohydrate antibody 2G12.
Virology 2007;360(2):294-304.
2007: Balzarini Jan; Van Damme Lut
Microbicide drug candidates to prevent HIV infection.
Lancet 2007;369(9563):787-97.
2007: Ducho Christian; Görbig Ulf; Jessel Sönke; Gisch Nicolas; Balzarini Jan; Meier Chris
Bis-cycloSal-d4T-monophosphates: drugs that deliver two molecules of bioactive nucleotides.
Journal of medicinal chemistry 2007;50(6):1335-46.
2007: Krecmerová Marcela; Holý Antonín; Pískala Alois; Masojídková Milena; Andrei Graciela; Naesens Lieve; Neyts Johan; Balzarini Jan; De Clercq Erik; Snoeck Robert
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: Chitneni Satish K; Deroose Christophe M; Balzarini Jan; Gijsbers Rik; Celen Sofie J L; de Groot Tjibbe J; Debyser Zeger; Mortelmans Luc; Verbruggen Alfons M; Bormans Guy M
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: Pati Hari N; Das Umashankar; De Clercq Erik; Balzarini Jan; Dimmock Jonathan R
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: Ji Lei; Chen Fen-Er; Xie Bin; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Balzarini Jan; Schols Dominique; Van Laethem Kristel; De Clercq Erik; Hocková Dana; Masojidkova Milina; Holý Antonin
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: Gazivoda Tatjana; Raic-Malic Silvana; Marjanovic Marko; Kralj Marijeta; Pavelic Kresimir; Balzarini Jan; De Clercq Erik; Mintas Mladen
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: Balzarini Jan; Van Herrewege Yven; Vermeire Kurt; Vanham Guido; Schols Dominique
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: Balzarini Jan; Van Laethem Kristel; Daelemans Dirk; Hatse Sigrid; Bugatti Antonella; Rusnati Marco; Igarashi Yasuhiro; Oki Toshikazu; Schols Dominique
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: Das Umashankar; Alcorn Jane; Shrivastav Anuraag; Sharma Rajendra K; De Clercq Erik; Balzarini Jan; Dimmock Jonathan R
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.
2007: Gisch N; Balzarini J; Meier C
5-diacetoxymethyl-cycloSal-d4TMP - A prototype of enzymatically activated cycloSal-pronucleotides.
Nucleosides, nucleotides & nucleic acids 2007;26(6-7):861-4.
2007: Görbig U; Balzarini J; Meier C
New cycloAmb-nucleoside phosphonate prodrugs.
Nucleosides, nucleotides & nucleic acids 2007;26(6-7):831-4.
2007: de Castro Sonia; Andrei Graziela; Snoeck Robert; Balzarini Jan; Camarasa María-José; Velázquez Sonsoles
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: Maruyama Tokumi; Demizu Yosuke; Kozai Shigetada; Witvrouw Myriam; Pannecouque Christophe; Balzarini Jan; Snoecks Robert; Andrei Graciella; De Clercq Erik
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: Roy Vincent; Kumamoto Hiroki; Berteina-Raboin Sabine; Nolan Steven P; Topalis Dimitri; Deville-Bonne Dominique; Balzarini Jan; Neyts Johan; Andrei Gracelia; Snoeck Robert; Agrofoglio Luigi A
Cross-metathesis mediated synthesis of new acyclic nucleoside phosphonates.
Nucleosides, nucleotides & nucleic acids 2007;26(10-12):1399-402.
2007: Broggi Julie; Joubert Nicolas; Aucagne Vincent; Berteina-Raboin Sabine; Diez-Gonzalez S; Nolan Steve; Topalis Dimitri; Deville-Bonne Dominique; Balzarini Jan; Neyts Johan; Andrei Graciela; Snoeck Robert; Agrofoglio Luigi A
Alkyne-azide click chemistry mediated carbanucleosides synthesis.
Nucleosides, nucleotides & nucleic acids 2007;26(10-12):1391-4.
2007: Vukadinovic-Tenter Dalibor; Balzarini Jan; Meier Chris
New developments of the "lock-in" modified cycloSal-d4TMPs.
Nucleosides, nucleotides & nucleic acids 2007;26(10-12):1325-8.
2007: Saïdi Hela; Nasreddine Nadine; Jenabian Mohammad-Ali; Lecerf Maxime; Schols Dominique; Krief Corinne; Balzarini Jan; Bélec Laurent
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: Liu Jiwei; Xu Xiaochao; Liu Jinzhi; Balzarini Jan; Luo Yongtin; Kong Yang; Li Jian; Chen Fang; Van Damme Els; Bao Jinku
A novel tetrameric lectin from Lycoris aurea with four mannose binding sites per monomer.
Acta biochimica Polonica 2007;54(1):159-66.
2007: Balzarini Jan
Carbohydrate-binding agents: a potential future cornerstone for the chemotherapy of enveloped viruses?
Antiviral chemistry & chemotherapy 2007;18(1):1-11.
2006: Barral Karine; Priet Stéphane; Sire Joséphine; Neyts Johan; Balzarini Jan; Canard Bruno; Alvarez Karine
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: Hernandez Ana-Isabel; Familiar Olga; Negri Ana; Rodríguez-Barrios Fatima; Gago Federico; Karlsson Anna; Camarasa María-José; Balzarini Jan; Pérez-Pérez María-Jesús
N1-substituted thymine derivatives as mitochondrial thymidine kinase (TK-2) inhibitors.
Journal of medicinal chemistry 2006;49(26):7766-73.
2006: Kristafor Vedran; Raic-Malic Silvana; Cetina Mario; Kralj Marijeta; Suman Lidija; Pavelic Kresimir; Balzarini Jan; De Clercq Erik; Mintas Mladen
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: McGuigan Christopher; Hassan-Abdallah Alshaimaa; Srinivasan Sheila; Wang Yikang; Siddiqui Adam; Daluge Susan M; Gudmundsson Kristjan S; Zhou Huiqiang; McLean Ed W; Peckham Jennifer P; Burnette Thimysta C; Marr Harry; Hazen Richard; Condreay Lynn D; Johnson Lance; Balzarini Jan
Application of phosphoramidate ProTide technology significantly improves antiviral potency of carbocyclic adenosine derivatives.
Journal of medicinal chemistry 2006;49(24):7215-26.
2006: Aquaro Stefano; Svicher Valentina; Schols Dominique; Pollicita Michela; Antinori Andrea; Balzarini Jan; Perno Carlo Federico
Mechanisms underlying activity of antiretroviral drugs in HIV-1-infected macrophages: new therapeutic strategies.
Journal of leukocyte biology 2006;80(5):1103-10.
2006: Romagnoli Romeo; Baraldi Pier Giovanni; Remusat Vincent; Carrion Maria Dora; Cara Carlota Lopez; Preti Delia; Fruttarolo Francesca; Pavani Maria Giovanna; Tabrizi Mojgan Aghazadeh; Tolomeo Manlio; Grimaudo Stefania; Balzarini Jan; Jordan Mary Ann; Hamel Ernest
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: El Omari Kamel; Bronckaers Annelies; Liekens Sandra; Pérez-Pérez Maria-Jésus; Balzarini Jan; Stammers David K
Structural basis for non-competitive product inhibition in human thymidine phosphorylase: implications for drug design.
The Biochemical journal 2006;399(2):199-204.
2006: Balzarini Jan; Keyaerts Els; Vijgen Leen; Egberink Herman; De Clercq Erik; Van Ranst Marc; Printsevskaya Svetlana S; Olsufyeva Eugenia N; Solovieva Svetlana E; Preobrazhenskaya Maria N
Inhibition of feline (FIPV) and human (SARS) coronavirus by semisynthetic derivatives of glycopeptide antibiotics.
Antiviral research 2006;72(1):20-33.
2006: Balzarini Jan
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: Ji Lei; Chen Fen-Er; Feng Xiao-Qing; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Casanova Elena; Hernandez Ana-Isabel; Priego Eva-María; Liekens Sandra; Camarasa María-José; Balzarini Jan; Pérez-Pérez María-Jesús
5'-O-tritylinosine and analogues as allosteric inhibitors of human thymidine phosphorylase.
Journal of medicinal chemistry 2006;49(18):5562-70.
2006: Balzarini Jan; Van Laethem Kristel; Peumans Willy J; Van Damme Els J M; Bolmstedt Anders; Gago Federico; Schols Dominique
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: Hatse Sigrid; Balzarini Jan; Liekens Sandra
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: Stevens Miguel; De Clercq Erik; Balzarini Jan
The regulation of HIV-1 transcription: molecular targets for chemotherapeutic intervention.
Medicinal research reviews 2006;26(5):595-625.
2006: Perno Carlo Federico; Svicher Valentina; Schols Dominique; Pollicita Michela; Balzarini Jan; Aquaro Stefano
Therapeutic strategies towards HIV-1 infection in macrophages.
Antiviral research 2006;71(2-3):293-300.
2006: Meier C; Balzarini J
Application of the cycloSal-prodrug approach for improving the biological potential of phosphorylated biomolecules.
Antiviral research 2006;71(2-3):282-92.
2006: McGuigan Christopher; Balzarini Jan
Aryl furano pyrimidines: the most potent and selective anti-VZV agents reported to date.
Antiviral research 2006;71(2-3):149-53.
2006: Balzarini J
Inhibition of HIV entry by carbohydrate-binding proteins.
Antiviral research 2006;71(2-3):237-47.
2006: García-Aparicio Carlos; Bonache María-Cruz; De Meester Ingrid; San-Félix Ana; Balzarini Jan; Camarasa María-José; Velazquez Sonsoles
Design and discovery of a novel dipeptidyl-peptidase IV (CD26)-based prodrug approach.
Journal of medicinal chemistry 2006;49(17):5339-51.
2006: Sluis-Cremer Nicolas; Hamamouch Noureddine; San Félix Ana; Velazquez Sonsoles; Balzarini Jan; Camarasa María-José
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: Liekens Sandra; Bronckaers Annelies; Hernández Ana-Isabel; Priego Eva-María; Casanova Elena; Camarasa Maria-José; Pérez-Pérez Maria-Jesus; Balzarini Jan
5'-O-tritylated nucleoside derivatives: inhibition of thymidine phosphorylase and angiogenesis.
Molecular pharmacology 2006;70(2):501-9.
2006: de Castro Sonia; García-Aparicio Carlos; Van Laethem Kristel; Gago Federico; Lobatón Esther; De Clercq Erik; Balzarini Jan; Camarasa María-José; Velázquez Sonsoles
Discovery of TSAO derivatives with an unusual HIV-1 activity/resistance profile.
Antiviral research 2006;71(1):15-23.
2006: Balzarini Jan; Liekens Sandra; Solaroli Nicola; El Omari Kamel; Stammers David K; Karlsson Anna
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: El Omari Kamel; Liekens Sandra; Bird Louise E; Balzarini Jan; Stammers David K
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: Franzolin Elisa; Rampazzo Chiara; Pérez-Pérez María-Jesús; Hernández Ana-Isabel; Balzarini Jan; Bianchi Vera
Bromovinyl-deoxyuridine: A selective substrate for mitochondrial thymidine kinase in cell extracts.
Biochemical and biophysical research communications 2006;344(1):30-6.
2006: Das Umashankar; Gul H Inci; Alcorn Jane; Shrivastav Anuraag; George Theresa; Sharma Rajendra K; Nienaber Kurt H; De Clercq Erik; Balzarini Jan; Kawase Masami; Kan Noriyuki; Tanaka Toru; Tani Satoru; Werbovetz Karl A; Yakovich Adam J; Manavathu Elias K; Stables James P; Dimmock Jonathan R
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: Ostrowski Tomasz; Golankiewicz Bozenna; De Clercq Erik; Balzarini Jan
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: Stevens Miguel; Pannecouque Christophe; De Clercq Erik; Balzarini Jan
Pyridine N-oxide derivatives inhibit viral transactivation by interfering with NF-kappaB binding.
Biochemical pharmacology 2006;71(8):1122-35.
2006: Maruyama Tokumi; Kozai Shigetada; Demizu Yosuke; Witvrouw Myriam; Pannecouque Christophe; Balzarini Jan; Snoecks Robert; Andrei Graciella; De Clercq Erik
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: Balzarini Jan; Keyaerts Els; Vijgen Leen; Vandermeer Frank; Stevens Miguel; De Clercq Erik; Egberink Herman; Van Ranst Marc
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: An Jie; Liu Jin-Zhi; Wu Chuan-Fang; Li Jian; Dai Lei; Van Damme Els; Balzarini Jan; De Clercq Erik; Chen Fang; Bao Jin-Ku
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: Robins Morris J; Miranda Karl; Rajwanshi Vivek K; Peterson Matt A; Andrei Graciela; Snoeck Robert; De Clercq Erik; Balzarini Jan
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: Barral Karine; Balzarini Jan; Neyts Johan; De Clercq Erik; Hider Robert C; Camplo Michel
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: Rajic Zrinka; Zorc Branka; Raic-Malic Silvana; Ester Katja; Kralj Marijeta; Pavelic Kresimir; Balzarini Jan; De Clercq Erik; Mintas Mladen
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: Liekens S; Balzarini J; Hernández A I; De Clercq E; Priego E M; Camarasa M J; Pérez-Pérez M J
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: El Omari Kamel; Solaroli Nicola; Karlsson Anna; Balzarini Jan; Stammers David K
Structure of vaccinia virus thymidine kinase in complex with dTTP: insights for drug design.
BMC structural biology 2006;6():22.
2006: Proost Paul; Struyf Sofie; Loos Tamara; Gouwy Mieke; Schutyser Evemie; Conings René; Ronsse Isabelle; Parmentier Marc; Grillet Bernard; Opdenakker Ghislain; Balzarini Jan; Van Damme Jo
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: Balzarini Jan; Celen Sofie; Karlsson Anna; de Groot Tjibbe; Verbruggen Alfons; Bormans Guy
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: Pérez-Pérez María-Jesús; Priego Eva-María; Hernández Ana-Isabel; Camarasa María-José; Balzarini Jan; Liekens Sandra
Thymidine phosphorylase inhibitors: recent developments and potential therapeutic applications.
Mini reviews in medicinal chemistry 2005;5(12):1113-23.
2005: Topalis Dimitri; Collinet Bruno; Gasse Cécile; Dugué Laurence; Balzarini Jan; Pochet Sylvie; Deville-Bonne Dominique
Substrate specificity of vaccinia virus thymidylate kinase.
The FEBS journal 2005;272(24):6254-65.
2005: Meier Chris; Görbig Ulf; Müller Christian; Balzarini Jan
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: Balzarini Jan; Van Laethem Kristel; Hatse Sigrid; Froeyen Matheus; Peumans Willy; Van Damme Els; Schols Dominique
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: Balzarini Jan
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: Turville Stuart G; Vermeire Kurt; Balzarini Jan; Schols Dominique
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: Stevens Miguel; Balzarini Jan; Tabarrini Oriana; Andrei Graciela; Snoeck Robert; Cecchetti Violetta; Fravolini Arnaldo; De Clercq Erik; Pannecouque Christophe
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: Bonache María-Cruz; Chamorro Cristina; Velázquez Sonsoles; De Clercq Erik; Balzarini Jan; Barrios Fátima Rodríguez; Gago Federico; Camarasa María-José; San-Félix Ana
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: Sun Guang-Fu; Kuang Yun-Yan; Chen Fen-Er; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Romagnoli Romeo; Baraldi Pier Giovanni; Jung M Katherine; Iaconinoto Maria Antonietta; Carrion Maria Dora; Remusat Vincent; Preti Delia; Tabrizi Mojgan Aghazadeh; Francesca Fruttarolo; De Clercq Erik; Balzarini Jan; Hamel Ernest
Synthesis and preliminary biological evaluation of new anti-tubulin agents containing different benzoheterocycles.
Bioorganic & medicinal chemistry letters 2005;15(18):4048-52.
2005: Auwerx Joeri; Rodríguez-Barrios Fátima; Ceccherini-Silberstein Francesca; San-Félix Ana; Velázquez Sonsoles; De Clercq Erik; Camarasa María-José; Perno Carlo-Federico; Gago Federico; Balzarini Jan
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: Sun Guang-Fu; Chen Xu-Xiang; Chen Fen-Er; Wang Yue-Ping; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Ceccherini-Silberstein Francesca; Gago Federico; Santoro Maria; Gori Caterina; Svicher Valentina; Rodríguez-Barrios Fátima; d'Arrigo Roberta; Ciccozzi Massimo; Bertoli Ada; d'Arminio Monforte Antonella; Balzarini Jan; Antinori Andrea; Perno Carlo-Federico
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: Bertoli Ada; Franco Maribel; Balzarini Jan; Johansson Magnus; Karlsson Anna
Altered deoxyribonucleotide pools in T-lymphoblastoid cells expressing the multisubstrate nucleoside kinase of Drosophila melanogaster.
The FEBS journal 2005;272(15):3918-28.
2005: Luoni Giovanna; McGuigan Christopher; Andrei Graciela; Snoeck Robert; De Clercq Erik; Balzarini Jan
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: Marchesan Silvia; Da Ros Tatiana; Spalluto Giampiero; Balzarini Jan; Prato Maurizio
Anti-HIV properties of cationic fullerene derivatives.
Bioorganic & medicinal chemistry letters 2005;15(15):3615-8.
2005: Breuer Michael; De Loof Arnold; Balzarini Jan; Huybrechts Roger
Insecticidal activity of the pyrimidine nucleoside analogue (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU).
Pest management science 2005;61(8):737-41.
2005: Janeba Zlatko; Balzarini Jan; Andrei Graciela; Snoeck Robert; De Clercq Erik; Robins Morris J
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: Balzarini Jan; Auwerx Joeri; Rodríguez-Barrios Fátima; Chedad Allel; Farkas Viktor; Ceccherini-Silberstein Francesca; García-Aparicio Carlos; Velázquez Sonsoles; De Clercq Erik; Perno Carlo-Federico; Camarasa María-José; Gago Federico
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: Nguyen Van Nhien Albert; Tomassi Cyrille; Len Christophe; Marco-Contelles José Luis; Balzarini Jan; Pannecouque Christophe; De Clercq Erik; Postel Denis
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: Printsevskaya Svetlana S; Solovieva Svetlana E; Olsufyeva Eugenia N; Mirchink Elena P; Isakova Elena B; De Clercq Erik; Balzarini Jan; Preobrazhenskaya Maria N
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: Aquaro Stefano; Svicher Valentina; Ceccherini-Silberstein Francesca; Cenci Alessandra; Marcuccilli Fabbio; Giannella Sara; Marcon Luisa; Caliò Raffaele; Balzarini Jan; Perno Carlo-Federico
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: Rodríguez-Barrios Fátima; Balzarini Jan; Gago Federico
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: McGuigan Christopher; Harris Sarah A; Daluge Susan M; Gudmundsson Kristjan S; McLean Ed W; Burnette Thimysta C; Marr Harry; Hazen Richard; Condreay Lynn D; Johnson Lance; De Clercq Erik; Balzarini Jan
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: Barreca Maria Letizia; Rao Angela; De Luca Laura; Zappalà Maria; Monforte Anna-Maria; Maga Giovanni; Pannecouque Christophe; Balzarini Jan; De Clercq Erik; Chimirri Alba; Monforte Pietro
Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT.
Journal of medicinal chemistry 2005;48(9):3433-7.
2005: Andrei Graciela; Balzarini Jan; Fiten Pierre; De Clercq Erik; Opdenakker Ghislain; Snoeck Robert
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: Balzarini Jan; Van Laethem Kristel; Hatse Sigrid; Froeyen Matheus; Van Damme Els; Bolmstedt Anders; Peumans Willy; De Clercq Erik; Schols Dominique
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: Auwerx Joeri; Van Nieuwenhove Joke; Rodríguez-Barrios Fátima; de Castro Sonia; Velázquez Sonsoles; Ceccherini-Silberstein Francesca; De Clercq Erik; Camarasa María-José; Perno Carlo-Federico; Gago Federico; Balzarini Jan
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: Gerona-Navarro Guillermo; Pérez de Vega M Jesús; García-López M Teresa; Andrei Graciela; Snoeck Robert; De Clercq Erik; Balzarini Jan; González-Muñiz Rosario
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: Andrei Graciela; Sienaert Rebecca; McGuigan Chris; De Clercq Erik; Balzarini Jan; Snoeck Robert
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: Naesens L; Lenaerts L; Andrei G; Snoeck R; Van Beers D; Holy Antonin; Balzarini Jan; De Clercq Erik
Antiadenovirus activities of several classes of nucleoside and nucleotide analogues.
Antimicrobial agents and chemotherapy 2005;49(3):1010-6.
2005: Ostrowski Tomasz; Golankiewicz Bozenna; De Clercq Erik; Balzarini Jan
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: de Castro Sonia; Lobatón Esther; Pérez-Pérez María-Jesús; San-Félix Ana; Cordeiro Alessandra; Andrei Graciela; Snoeck Robert; De Clercq Erik; Balzarini Jan; Camarasa María-José; Velázquez Sonsoles
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: Balzarini Jan; Van Damme Lut
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: Barbaric Monika; Ursic Stanko; Pilepic Viktor; Zorc Branka; Hergold-Brundic Antonija; Nagl Ante; Grdisa Mira; Pavelic Kresimir; Snoeck Robert; Andrei Graciela; Balzarini Jan; De Clercq Erik; Mintas Mladen
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: Leyssen Pieter; Balzarini Jan; De Clercq Erik; Neyts Johan
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: Balzarini Jan; Stevens Miguel; De Clercq Erik; Schols Dominique; Pannecouque Christophe
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: Opacic Ninoslav; Barbaric Monika; Zorc Branka; Cetina Mario; Nagl Ante; Frkovic Danijel; Kralj Marijeta; Pavelic Kresimir; Balzarini Jan; Andrei Graciela; Snoeck Robert; De Clercq Erik; Raic-Malic Silvana; Mintas Mladen
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: Barral Karine; Courcambeck Jérôme; Pèpe Gérard; Balzarini Jan; Neyts Johan; De Clercq Erik; Camplo Michel
Synthesis and antiviral evaluation of cis-substituted cyclohexenyl and cyclohexanyl nucleosides.
Journal of medicinal chemistry 2005;48(2):450-6.
2005: Andersson Elin; Horal Peter; Jejcic Alenka; Höglund Stefan; Balzarini Jan; Vahlne Anders; Svennerholm Bo
Glycine-amide is an active metabolite of the antiretroviral tripeptide glycyl-prolyl-glycine-amide.
Antimicrobial agents and chemotherapy 2005;49(1):40-4.
2005: Gazivoda Tatjana; Plevnik Miha; Plavec Janez; Kraljevic Sandra; Kralj Marijeta; Pavelic Kresimir; Balzarini Jan; De Clercq Erik; Mintas Mladen; Raic-Malic Silvana
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: Zhou Longhu; Amer Adel; Korn Michael; Burda Robert; Balzarini Jan; De Clercq Erik; Kern Earl R; Torrence Paul F
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: Pérez-Pérez María-Jesús; Hernández Ana-Isabel; Priego Eva-María; Rodríguez-Barrios Fátima; Gago Federico; Camarasa María-José; Balzarini Jan
Mitochondrial thymidine kinase inhibitors.
Current topics in medicinal chemistry 2005;5(13):1205-19.
2005: Vukadinovic D; Böge N P H; Balzarini J; Meier C
"Lock-in" modified cyclosal nucleotides--the second generation of cyclosal prodrugs.
Nucleosides, nucleotides & nucleic acids 2005;24(5-7):939-42.
2005: Kelleher M R; McGuigan C; Bidet O; Carangio A; Weldon H; Andrei G; Snoeck R; De Clercq E; Balzarini J
The journey towards elucidating the anti-HCMV activity of alkylated bicyclic furano pyrimidines.
Nucleosides, nucleotides & nucleic acids 2005;24(5-7):643-5.
2005: Goslinski Tomasz; Januszczyk Piotr; Wenska Grazyna; Golankiewicz Bozenna; De Clercq Erik; Balzarini Jan
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: Ducho C; Jessel S; Gisch N; Balzarini J; Meier C
Novel cyclosal nucleotides with reduced inhibitory potency toward human butyrylcholinesterase.
Nucleosides, nucleotides & nucleic acids 2005;24(5-7):519-22.
2005: De Clercq Erik; Andrei G; Balzarini J; Leyssen P; Naesens L; Neyts J; Pannecouque C; Snoeck R; Ying C; Hocková D; Holý A
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: Prekupec Svjetlana; Makuc Damjan; Plavec Janez; Kraljevic Sandra; Kralj Marijeta; Pavelic Kresimir; Andrei Graciela; Snoeck Robert; Balzarini Jan; De Clercq Erik; Raic-Malic Silvana; Mintas Mladen
Antiviral and cytostatic evaluation of the novel 6-acyclic chain substituted thymine derivatives.
Antiviral chemistry & chemotherapy 2005;16(5):327-38.
2004: Orzeszko Barbara; Kazimierczuk Zygmunt; Maurin Jan Krzysztof; Laudy Agnieszka Ewa; Starosciak Bohdan Jerzy; Vilpo Juhani; Vilpo Leena; Balzarini Jan; Orzeszko Andrzej
Novel adamantylated pyrimidines and their preliminary biological evaluations.
Farmaco (Società chimica italiana : 1989) 2004;59(12):929-37.
2004: He Yanping; Chen Fener; Yu Xiongjie; Wang Yueping; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Luoni Giovanna M; McGuigan Christopher; Andrei Graciela; Snoeck Robert; De Clercq Erik; Balzarini Jan
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: Bidet Olivier; McGuigan Christopher; Snoeck Robert; Andrei Graciela; De Clercq Erik; Balzarini Jan
Non-nucleoside structures retain full anti-HCMV potency of the dideoxy furanopyrimidine family.
Antiviral chemistry & chemotherapy 2004;15(6):329-32.
2004: Balzarini J; Pannecouque C; Naesens L; Andrei G; Snoeck R; De Clercq E; Hocková D; Holý A
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: Maslen Hannah L; Hughes David; Hursthouse Mike; De Clercq Erik; Balzarini Jan; Simons Claire
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: Balzarini Jan; Hatse Sigrid; Vermeire Kurt; Princen Katrien; Aquaro Stefano; Perno Carlo-Federico; De Clercq Erik; Egberink Herman; Vanden Mooter Guy; Peumans Willy; Van Damme Els; Schols Dominique
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: Balzarini Jan; Van Laethem Kristel; Hatse Sigrid; Vermeire Kurt; De Clercq Erik; Peumans Willy; Van Damme Els; Vandamme Anne-Mieke; Bölmstedt Anders; Schols Dominique;
Profile of resistance of human immunodeficiency virus to mannose-specific plant lectins.
Journal of virology 2004;78(19):10617-27.
2004: Priego Eva-María; Balzarini Jan; Karlsson Anna; Camarasa María-José; Pérez-Pérez María-Jesús
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: Balzarini Jan; Andersson Elin; Schols Dominique; Proost Paul; Van Damme Jo; Svennerholm Bo; Horal Peter; Vahlne Anders
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: Balzarini Jan; Aquaro Stefano; Hassan-Abdallah Alshaimaa; Daluge Susan M; Perno Carlo-Federico; McGuigan Chris
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: Rao A; Balzarini J; Carbone A; Chimirri A; De Clercq E; Monforte A M; Monforte P; Pannecouque C; Zappalà M
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: Kifli Nurolaini; De Clercq Erik; Balzarini Jan; Simons Claire
Novel imidazo[1,2-c]pyrimidine base-modified nucleosides: synthesis and antiviral evaluation.
Bioorganic & medicinal chemistry 2004;12(15):4245-52.
2004: Auwerx Joeri; Stevens Miguel; Van Rompay An R; Bird Louise E; Ren Jingshan; De Clercq Erik; Oberg Bo; Stammers David K; Karlsson Anna; Balzarini Jan
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: Liekens Sandra; Hernández Ana-Isabel; Ribatti Domenico; De Clercq Erik; Camarasa María-José; Pérez-Pérez María-Jesús; Balzarini Jan
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: Velázquez Sonsoles; Lobatón Esther; De Clercq Erik; Koontz Dianna L; Mellors John W; Balzarini Jan; Camarasa María-José
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: Kifli Nurolaini; Thet Htar Thet; De Clercq Erik; Balzarini Jan; Simons Claire
Novel bicyclic sugar modified nucleosides: synthesis, conformational analysis and antiviral evaluation.
Bioorganic & medicinal chemistry 2004;12(12):3247-57.
2004: Hocková Dana; Holý Antonín; Masojídková Milena; Andrei Graciela; Snoeck Robert; De Clercq Erik; Balzarini Jan
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: He Yanping; Chen Fener; Sun Guangfu; Wang Yueping; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Baraldi Pier Giovanni; Del Carmen Nunez Maria; Tabrizi Mojgan Aghazadeh; De Clercq Erik; Balzarini Jan; Bermejo Jaime; Estévez Francisco; Romagnoli Romeo
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: Meier Chris; Ducho Christian; Görbig Ulf; Esnouf Robert; Balzarini Jan
Interaction of cycloSal-pronucleotides with cholinesterases from different origins. A structure-activity relationship.
Journal of medicinal chemistry 2004;47(11):2839-52.
2004: Meier Chris; Ruppel Manuel F H; Vukadinovic Dalibor; Balzarini Jan
"Lock-in"-cycloSal-pronucleotides - a new generation of chemical Trojan Horses?
Mini reviews in medicinal chemistry 2004;4(4):383-94.
2004: Cahard Dominique; McGuigan Christopher; Balzarini Jan
Aryloxy phosphoramidate triesters as pro-tides.
Mini reviews in medicinal chemistry 2004;4(4):371-81.
2004: Angell Annette; McGuigan Christopher; Garcia Sevillano Luis; Snoeck Robert; Andrei Graciela; De Clercq Erik; Balzarini Jan
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: Gerona-Navarro Guillermo; Pérez de Vega M Jesús; García-López M Teresa; Andrei Graciela; Snoeck Robert; Balzarini Jan; De Clercq Erik; González-Muñiz Rosario
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: Rinaldo-Matthis Agnes; Rampazzo Chiara; Balzarini Jan; Reichard Peter; Bianchi Vera; Nordlund Pär
Crystal structures of the mitochondrial deoxyribonucleotidase in complex with two specific inhibitors.
Molecular pharmacology 2004;65(4):860-7.
2004: Borst P; Balzarini J; Ono N; Reid G; de Vries H; Wielinga P; Wijnholds J; Zelcer N
The potential impact of drug transporters on nucleoside-analog-based antiviral chemotherapy.
Antiviral research 2004;62(1):1-7.
2004: McGuigan Christopher; Pathirana Ranjith N; Snoeck Robert; Andrei Graciela; De Clercq Erik; Balzarini Jan
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: Sienaert R; Andrei G; Snoeck R; De Clercq E; McGuigan C; Balzarini J
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: Raic-Malic Silvana; Tomaskovic Linda; Mrvos-Sermek Draginja; Prugovecki Biserka; Cetina Mario; Grdisa Mira; Pavelic Kresimir; Mannschreck Albrecht; Balzarini Jan; De Clercq Erik; Mintas Mladen
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: Dimmock J R; Chamankhah M; Das U; Zello G A; Quail J W; Yang J; Nienaber K H; Sharma R K; Selvakumar P; Balzarini J; De Clercq E; Stables J P
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: Vashishtha Sarvesh C; Zello Gordon A; Nienaber Kurt H; Balzarini Jan; De Clercq Erik; Stables James P; Dimmock Jonathan R
Cytotoxic and anticonvulsant aryloxyaryl Mannich bases and related compounds.
European journal of medicinal chemistry 2004;39(1):27-35.
2004: Meier Chris; Meerbach Astrid; Balzarini Jan
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: Rao Angela; Balzarini Jan; Carbone Anna; Chimirri Alba; De Clercq Erik; Monforte Anna Maria; Monforte Pietro; Pannecouque Christophe; Zappalà Maria
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: Rosen Thomas C; De Clercq Erik; Balzarini Jan; Haufe Günter
Synthesis and antiviral activity of monofluorinated cyclopropanoid nucleosides.
Organic & biomolecular chemistry 2004;2(2):229-37.
2004: Auwerx Joeri; Esnouf Robert; De Clercq Erik; Balzarini Jan
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: Mendieta Jesús; Martín-Santamaría Sonsoles; Priego Eva-María; Balzarini Jan; Camarasa María-José; Pérez-Pérez María-Jesús; Gago Federico
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: Van Herrewege Yven; Michiels Jo; Van Roey Jens; Fransen Katrien; Kestens Luc; Balzarini Jan; Lewi Paul; Vanham Guido; Janssen Paul
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.
2004: Maruyama Tokumi; Kozai Shigetada; Demizu Yosuke; Witvrouw Myriam; Pannecouque Christophe; Balzarini Jan; Snoeck Robert; Andrei Graciella; De Clercq Erik
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: Voss Jürgen; Wirsching Jörn; Schulze Oliver; Adiwidjaja Gunadi; Giesler Anja; Balzarini Jan; De Clercq Erik
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: Chatgilialoglu Chryssostomos; Ferreri Carla; Gimisis Thanasis; Roberti Marinella; Balzarini Jan; De Clercq Erik
Synthesis and biological evaluation of novel 1'-branched and spironucleoside analogues.
Nucleosides, nucleotides & nucleic acids 2004;23(10):1565-81.
2004: Perno C-F; Balestra E; Francesconi M; Abdelahad D; Caliò R; Balzarini J; Aquaro S
Antiviral profile of HIV inhibitors in macrophages: implications for therapy.
Current topics in medicinal chemistry 2004;4(9):1009-15.
2004: Camarasa María-José; San-Félix Ana; Velázquez Sonsoles; Pérez-Pérez María-Jesús; Gago Federico; Balzarini Jan
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: Balzarini J
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: Meier Chris; Ruppel Manuel F H; Vukadinovic Dalibor; Balzarini Jan
Second generation of cycloSal-pronucleotides with esterase-cleavable sites: the "lock-in"-concept.
Nucleosides, nucleotides & nucleic acids 2004;23(1-2):89-115.
2004: Jaksa Suzana; Kralj Bogdan; Pannecouque Christophe; Balzarini Jan; De Clercq Erik; Kobe Joze
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: Kumar Piyush; Ohkura Kazue; Balzarini Jan; De Clercq Erik; Seki Koh-ichi; Wiebe Leonard I
Synthesis and antiviral activity of novel fluorinated 2',3'-dideoxynucleosides.
Nucleosides, nucleotides & nucleic acids 2004;23(1-2):7-29.
2004: McGuigan Christopher; Carangio Antonella; Snoeck Robert; Andrei Graciela; De Clercq Erik; Balzarini Jan
Synthesis and antiviral evaluation of some 3'-fluoro bicyclic nucleoside analogues.
Nucleosides, nucleotides & nucleic acids 2004;23(1-2):1-5.
2003: Prekupec Svjetlana; Svedruzic Drazenka; Gazivoda Tatjana; Mrvos-Sermek Draginja; Nagl Ante; Grdisa Mira; Pavelic Kresimir; Balzarini Jan; De Clercq Erik; Folkers Gerd; Scapozza Leonardo; Mintas Mladen; Raic-Malic Silvana
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: McGuigan Christopher; Brancale Andrea; Andrei Graciela; Snoeck Robert; De Clercq Erik; Balzarini Jan
Novel bicyclic furanopyrimidines with dual anti-VZV and -HCMV activity.
Bioorganic & medicinal chemistry letters 2003;13(24):4511-3.
2003: Bosi Susanna; Da Ros Tatiana; Spalluto Giampiero; Balzarini Jan; Prato Maurizio
Synthesis and anti-HIV properties of new water-soluble bis-functionalized[60]fullerene derivatives.
Bioorganic & medicinal chemistry letters 2003;13(24):4437-40.
2003: Barral Karine; Hider Robert C; Balzarini Jan; Neyts Johan; De Clercq Erik; Camplo Michel
Synthesis and antiviral evaluation of 3-hydroxy-2-methylpyridin-4-one dideoxynucleoside derivatives.
Bioorganic & medicinal chemistry letters 2003;13(24):4371-4.
2003: Hocková Dana; Holý Antonín; Masojídková Milena; Andrei Graciela; Snoeck Robert; De Clercq Erik; Balzarini Jan
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: Wirsching Jörn; Voss Jürgen; Giesler Anja; Kopf Jürgen; Adiwidjaja Gunadi; Balzarini Jan; De Clercq Erik
Thiosugars. X. Novel nucleoside analogues derived from 4-thio-L-lyxofuranose.
Nucleosides, nucleotides & nucleic acids 2003;22(10):1867-97.
2003: Stevens Miguel; Pannecouque Christophe; De Clercq Erik; Balzarini Jan
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: Maruyama Tokumi; Kozai Shigetada; Yamasaki Tetsuo; Witvrouw Myriam; Pannecouque Christophe; Balzarini Jan; Snoeck Robert; Andrei Graciella; De Clercq Erik
Synthesis and antiviral activity of 1,3-disubstituted uracils against HIV-1 and HCMV.
Antiviral chemistry & chemotherapy 2003;14(5):271-9.
2003: Bonache María-Cruz; Chamorro Cristina; Lobatón Esther; De Clercq Erik; Balzarini Jan; Velázquez Sonsoles; Camarasa María-José; San-Félix Ana
Structure-activity relationship studies on a novel family of specific HIV-1 reverse transcriptase inhibitors.
Antiviral chemistry & chemotherapy 2003;14(5):249-62.
2003: Blanco José Manuel; Caamaño Olga; Fernández Franco; Rodríguez-Borges José Enrique; Balzarini Jan; de Clercq Erik
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: Hernández Ana-Isabel; Balzarini Jan; Rodríguez-Barrios Fátima; San-Félix Ana; Karlsson Anna; Gago Federico; Camarasa María-José; Pérez-Pérez María Jesús
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: Stevens Miguel; Pannecouque Christophe; De Clercq Erik; Balzarini Jan
Inhibition of human immunodeficiency virus by a new class of pyridine oxide derivatives.
Antimicrobial agents and chemotherapy 2003;47(9):2951-7.
2003: Dimmock J R; Jha A; Zello G A; Sharma R K; Shrivastav A; Selvakumar P; Allen T M; Santos C L; Balzarini J; De Clercq E; Manavathu E K; Stables J P
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: Dimmock J R; Padmanilayam M P; Das U; Zello G A; Sharma R K; Shrivastav A; Selvakumar P; Pasha M K; Nienaber K H; Lee J S; Allen T M; Santos C L; Balzarini J; De Clercq E
Cytotoxic mannich bases of 1-arylidene-2-tetralones.
Journal of enzyme inhibition and medicinal chemistry 2003;18(4):313-24.
2003: Mazzon Cristina; Rampazzo Chiara; Scaini Maria Chiara; Gallinaro Lisa; Karlsson Anna; Meier Chris; Balzarini Jan; Reichard Peter; Bianchi Vera
Cytosolic and mitochondrial deoxyribonucleotidases: activity with substrate analogs, inhibitors and implications for therapy.
Biochemical pharmacology 2003;66(3):471-9.
2003: Manfredini Stefano; Solaroli Nicola; Angusti Angela; Nalin Federico; Durini Elisa; Vertuani Silvia; Pricl Sabrina; Ferrone Marco; Spadari Silvio; Focher Federico; Verri Annalisa; De Clercq Erik; Balzarini Jan
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: Galtier Christophe; Mavel Sylvie; Snoeck Robert; Andreï Graciela; Pannecouque Christophe; Witvrouw Myriam; Balzarini Jan; De Clercq Erik; Gueiffier Alain
Synthesis and antiviral activities of 3-aralkylthiomethylimidazo[1,2-b]pyridazine derivatives.
Antiviral chemistry & chemotherapy 2003;14(4):177-82.
2003: Choi Yongseok; George Clifford; Comin Maria J; Barchi Joseph J; Kim Hak Sung; Jacobson Kenneth A; Balzarini Jan; Mitsuya Hiroaki; Boyer Paul L; Hughes Stephen H; Marquez Victor E
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: Meng Ge; Chen Fen-Er; De Clercq Erik; Balzarini Jan; Pannecouque Christophe
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: Bird Louise E; Ren Jingshan; Wright Alan; Leslie Kris D; Degrève Bart; Balzarini Jan; Stammers David K
Crystal structure of varicella zoster virus thymidine kinase.
The Journal of biological chemistry 2003;278(27):24680-7.
2003: Spaepen Karoline; Stroobants Sigrid; Dupont Patrick; Vandenberghe Peter; Maertens Johan; Bormans Guy; Thomas José; Balzarini Jan; De Wolf-Peeters Christine; Mortelmans Luc; Verhoef Gregor
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: Balzarini Jan; Pannecouque Christophe; De Clercq Erik; Pavlov Andrey Y; Printsevskaya Svetlana S; Miroshnikova Olga V; Reznikova Marina I; Preobrazhenskaya Maria N
Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics.
Journal of medicinal chemistry 2003;46(13):2755-64.
2003: Roy Béatrice; Chambert Stéphane; Lepoivre Michel; Aubertin Anne-Marie; Balzarini Jan; Décout Jean-Luc
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: De Bolle L; Balzarini J; De Clercq E; Naesens L
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: Sienaert R; Naesens L; Brancale A; Carangio A; Andrei G; Snoeck R; Van Kuilenburg A; De Clercq E; McGuigan C; Balzarini J
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: de Castro Sonia; Pérez-Pérez María-Jesús; Lobatón Esther; De Clercq Erik; Balzarini Jan; Camarasa María-José; Velázquez Sonsoles
Unusual lability of 5'-O-tert-butyldimethylsilyl group on 4''-acyl TSAO derivatives.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):959-61.
2003: Priego E M; Mendieta J; Gago F; Balzarini J; De Clercq E; Camarasa M J; Pérez-Pérez M J
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: Bonache María-Cruz; Chamorro Cristina; Velázquez Sonsoles; De Clercq Erik; Balzarini Jan; Camarasa María-José; San-Félix Ana
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: Carangio A; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Luoni G; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
Bicyclic nucleoside inhibitors of varicella-zoster virus: 5'-chloro and 3'-chloro derivatives.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):931-3.
2003: Goslinski Tomasz; Wenska Grazyna; Golankiewicz Bozenna; Balzarini Jan; De Clercq Erik
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: Ermolinsky Boris S; Efimtseva Ekaterina V; Alexeev Cyrill S; Mikhailov Sergey N; Balzarini Jan; De Clercq Erik
Dinucleoside monophosphates containing AZT and 1-methyladenosine or 7-methylguanosine.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):853-5.
2003: Ducho C; Balzarini J; Meier C
Non-inhibition of acetylcholinesterase by cycloSal nucleotides.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):841-3.
2003: Meier C; Renze J T; Balzarini J; De Clercq E
d4TMP delivery from 7-substituted cycloSal-d4TMPs.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):825-7.
2003: Müller H C; Meier C; Balzarini J; Reinstein J
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: Bidet O; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Muus U; De Clercq E; Balzarini J; Naesens L; Meier C
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: Barai Vladimir N; Zinchenko Anatoli I; Eroshevskaya Ludmilla A; Zhernosek Elena V; Balzarini Jan; De Clercq Erik; Mikhailopulo Igor A
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: McGuigan Christopher; Jukes Alison; Blewett Sally; Barucki Hubert; Erichsen Jonathan T; Andrei Graciella; Snoeck Robert; De Clercq Erik; Balzarini Jan
Halophenyl furanopyrimidines as potent and selective anti-VZV agents.
Antiviral chemistry & chemotherapy 2003;14(3):165-70.
2003: Balzarini Jan; De Clercq Erik; Kaminska Beata; Orzeszko Andrzej
Synthesis and antiviral activity of some 5'-N-phthaloyl-3'-azido-2',3'-dideoxythymidine analogues.
Antiviral chemistry & chemotherapy 2003;14(3):139-44.
2003: Poznanski Jaroslaw; Bretner Maria; Kulikowski Tadeusz; Balzarini Jan; Van Aerschot Arthur; De Clercq Erik
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: Reid Glen; Wielinga Peter; Zelcer Noam; De Haas Marcel; Van Deemter Liesbeth; Wijnholds Jan; Balzarini Jan; Borst Piet
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: Spaepen Karoline; Stroobants Sigrid; Dupont Patrick; Bormans Guy; Balzarini Jan; Verhoef Gregor; Mortelmans Luc; Vandenberghe Peter; De Wolf-Peeters Christine
[(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: Dzolic Zoran; Kristafor Vedran; Cetina Mario; Nagl Ante; Hergold-Brundic Antonija; Mrvos-Sermek Draginja; Burgemeister Thomas; Grdisa Mira; Slade Neda; Pavelic Kresimir; Balzarini Jan; De Clercq Erik; Mintas Mladen
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: Dimmock J R; Jha A; Zello G A; Allen T M; Santos C L; Balzarini J; De Clercq E; Manavathu E K; Stables J P
Cytotoxic 4'-aminochalcones and related compounds.
Die Pharmazie 2003;58(4):227-32.
2003: Agbaria Riad; Manor Esther; Barak Jacob; Balzarini Jan
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: Lagoja Irene M; Pannecouque Christophe; Van Aerschot Arthur; Witvrouw Myriam; Debyser Zeger; Balzarini Jan; Herdewijn Piet; De Clercq Erik
N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action.
Journal of medicinal chemistry 2003;46(8):1546-53.
2003: Naimi Ebrahim; Zhou Aihua; Khalili Panteha; Wiebe Leonard I; Balzarini Jan; De Clercq Erik; Knaus Edward E
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: Dimmock Jonathan R; Padmanilayam Maniyan P; Zello Gordon A; Nienaber Kurt H; Allen Theresa M; Santos Cheryl L; De Clercq Erik; Balzarini Jan; Manavathu Elias K; Stables James P
Cytotoxic analogues of 2,6-bis(arylidene)cyclohexanones.
European journal of medicinal chemistry 2003;38(2):169-77.
2003: Balzarini Jan; Hernández Ana-Isabel; Roche Philippe; Esnouf Robert; Karlsson Anna; Camarasa Maria-José; Pérez-Pérez Maria-Jesus
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: Dimmock Jonathan R; Jha Amitabh; Zello Gordon A; Quail J Wilson; Oloo Eliud O; Nienaber Kurt H; Kowalczyk Earl S; Allen Theresa M; Santos Cheryl L; De Clercq Erik; Balzarini Jan; Manavathu Elias K; Stables James P
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: Guenther Sven; Balzarini Jan; De Clercq Erik; Nair Vasu
A thymidine phosphorylase-stable analogue of BVDU with significant antiviral activity.
Journal of medicinal chemistry 2002;45(25):5426-9.
2002: Barreca Maria L; Balzarini Jan; Chimirri Alba; De Clercq Erik; De Luca Laura; Höltje Hans Dieter; Höltje Monika; Monforte Anna Maria; Monforte Pietro; Pannecouque Christophe; Rao Angela; Zappalà Maria
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: Balzarini Jan; Van Herrewege Yven; Vanham Guido
Metabolic activation of nucleoside and nucleotide reverse transcriptase inhibitors in dendritic and Langerhans cells.
AIDS (London, England) 2002;16(16):2159-63.
2002: Goslinski Tomasz; Golankiewicz Bozenna; De Clercq Erik; Balzarini Jan
Synthesis and biological activity of strongly fluorescent tricyclic analogues of acyclovir and ganciclovir.
Journal of medicinal chemistry 2002;45(23):5052-7.
2002: Dimmock Jonathan R; Padmanilyam Maniyan P; Zello Gordon A; Quail J Wilson; Oloo Eliud O; Prisciak Jared S; Kraatz Heinz Bernhard; Cherkasov Arten; Lee Jeremy S; Allen Theresa M; Santos Cheryl L; Manavathu Elias K; De Clercq Erik; Balzarini Jan; Stables James P
Cytotoxic 1,3-diarylidene-2-tetralones and related compounds.
European journal of medicinal chemistry 2002;37(10):813-24.
2002: Van Herrewege Yven; Penne Lieve; Vereecken Chris; Fransen Katrien; van der Groen Guido; Kestens Luc; Balzarini Jan; Vanham Guido
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: Meiera Chris; Renzea Jürgen; Ducho Christian; Balzarini Jan
cycloSal-d4TMP pronucleotides structural variations, mechanistic insights and antiviral activity.
Current topics in medicinal chemistry 2002;2(10):1111-21.
2002: Carangio A; Srinivasan S; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Santana Lourdes; Teijeira Marta; Uriarte Eugenio; Balzarini Jan; De Clercq Erik
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: Hernández Ana-Isabel; Balzarini Jan; Karlsson Anna; Camarasa María-José; Pérez-Pérez María-Jesús
Acyclic nucleoside analogues as novel inhibitors of human mitochondrial thymidine kinase.
Journal of medicinal chemistry 2002;45(19):4254-63.
2002: Balzarini J; Ostrowski T; Goslinski T; De Clercq E; Golankiewicz B
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: Lobatón Esther; Rodríguez-Barrios Fátima; Gago Federico; Pérez-Pérez María-Jesús; De Clercq Erik; Balzarini Jan; Camarasa María-José; Velázquez Sonsoles
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: Aquaro Stefano; Caliò Raffaele; Balzarini Jan; Bellocchi Maria Concetta; Garaci Enrico; Perno Carlo Federico
Macrophages and HIV infection: therapeutical approaches toward this strategic virus reservoir.
Antiviral research 2002;55(2):209-25.
2002: Balzarini Jan; McGuigan Christopher
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: Dimmock Jonathan R; Zello Gordon A; Oloo Eliud O; Quail J Wilson; Kraatz Heinz-Bernhard; Perjési Pál; Aradi Ferenc; Takács-Novák Krisztina; Allen Theresa M; Santos Cheryl L; Balzarini Jan; De Clercq Erik; Stables James P
Correlations between cytotoxicity and topography of some 2-arylidenebenzocycloalkanones determined by X-ray crystallography.
Journal of medicinal chemistry 2002;45(14):3103-11.
2002: Balzarini J; McGuigan C
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: Balzarini J; Pannecouque C; De Clercq E; Aquaro S; Perno C-F; Egberink H; Holý A
Antiretrovirus activity of a novel class of acyclic pyrimidine nucleoside phosphonates.
Antimicrobial agents and chemotherapy 2002;46(7):2185-93.
2002: Manallack David T; Pitt Will R; Herdewijn Piet; Balzarini Jan; De Clercq Erik; Sanderson Mark R; Sohi Maninder; Wien Frank; Munier-Lehmann Helene; Haouz Ahmed; Delarue Marc
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: Balzarini Jan; Liekens Sandra; Esnouf Robert; De Clercq Erik
The A167Y mutation converts the herpes simplex virus type 1 thymidine kinase into a guanosine analogue kinase.
Biochemistry 2002;41(20):6517-24.
2002: Balzarini Jan; Sienaert Rebecca; Liekens Sandra; Van Kuilenburg André; Carangio Antonella; Esnouf Robert; De Clercq Erik; McGuigan Chris
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: Holý Antonín; Votruba Ivan; Masojídková Milena; Andrei Graciela; Snoeck Robert; Naesens Lieve; De Clercq Erik; Balzarini Jan
6-[2-(Phosphonomethoxy)alkoxy]pyrimidines with antiviral activity.
Journal of medicinal chemistry 2002;45(9):1918-29.
2002: Mavel Sylvie; Renou Jean-Louis; Galtier Christophe; Allouchi Hassan; Snoeck Robert; Andrei Graciella; De Clercq Erik; Balzarini Jan; Gueiffier Alain
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: McGuigan Christopher; Blewett Sally; Siccardi Dario; Erichsen Jonathan T; Andrei Graciela; Snoek Robert; De Clercq Erik; Balzarini Jan
Alkyloxyphenyl furano pyrimidines as potent and selective anti-VZV agents with enhanced water solubility.
Antiviral chemistry & chemotherapy 2002;13(2):91-9.
2002: Ducho Christian; Balzarini Jan; Naesens Lieve; De Clercq Erik; Meier Chris
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: Meier Chris; Muus Ulrike; Renze Jürgen; Naesens Lieve; De Clercq Erik; Balzarini Jan
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: Deferme S; Van Gelder J; Ingels F; Van den Mooter G; De Buck S; Balzarini J; Naesens L; De Clercq E; Kinget R; Augustijns P
Intestinal absorption characteristics of the low solubility thiocarboxanilide UC-781.
International journal of pharmaceutics 2002;234(1-2):113-9.
2002: Auwerx Joeri; North Thomas W; Preston Bradley D; Klarmann George J; De Clercq Erik; Balzarini Jan
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: Sienaert Rebecca; Naesens Lieve; Brancale Andrea; De Clercq Erik; McGuigan Christopher; Balzarini Jan
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: Das Subha R; Schneller Stewart W; Balzarini Jan; De Clercq Erik
A mercapto analogue of 5'-noraristeromycin.
Bioorganic & medicinal chemistry 2002;10(2):457-60.
2002: Dimmock Jonathan R; Jha Amitabh; Kumar Praveen; Zello Gordon A; Quail J Wilson; Oloo Eliud O; Oucharek Jennifer J; Pasha Mohammed K; Seitz Dallas; Sharma Rajendra K; Allen Theresa M; Santos Cheryl L; Manavathu Elias K; De Clercq Erik; Balzarini Jan; Stables James P
Cytotoxic 1,4-bis(2-oxo-1-cycloalkylmethylene)benzenes and related compounds.
European journal of medicinal chemistry 2002;37(1):35-44.
2002: Liekens Sandra; Bilsen Filip; De Clercq Erik; Priego Eva María; Camarasa María José; Pérez-Pérez María Jesús; Balzarini Jan
Anti-angiogenic activity of a novel multi-substrate analogue inhibitor of thymidine phosphorylase.
FEBS letters 2002;510(1-2):83-8.
2002: Wirsching Jörn; Schulze Oliver; Voss Jürgen; Giesler Anja; Kopf Jürgen; Adiwidjaja Gunadi; Balzarini Jan; De Clercq Erik
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: Nieto M Isabel; Caamaño Olga; Fernández Franco; Gómez Maria; Balzarini Jan; De Clercq Erik
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: Tronchet Jean M J; Chalard Frederic; Rivara-Minten Elisabeth; Seman Michel; De Clercq Erik; Balzarini Jan; Dilda Pierre
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.
2001: Tronchet J M; Kovacs I; Dilda P; Seman M; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Chaouni-Enabdallah A; Galtier C; Allouchi H; Kherbeche A; Chavignon O; Teulade J C; Witvrouw M; Pannecouque C; Snoeck R; Andrei G; Balzarini J; De Clercq E; Fauvelle F; Enguehard C; Gueiffier A
3-Benzamido, ureido and thioureidoimidazo[1,2-a]pyridine derivatives as potential antiviral agents.
Chemical & pharmaceutical bulletin 2001;49(12):1631-5.
2001: Chamorro C; Lobatón E; Bonache M C; De Clercq E; Balzarini J; Velázquez S; San-Félix A; Camarasa M J
Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.
Bioorganic & medicinal chemistry letters 2001;11(23):3085-8.
2001: Martinez A; Gil C; Castro A; Perez C; Witvrouw M; Pannecouque C; Balzarini J; De Clercq E
Anti-HIV-1 activity of benzothiadiazine dioxide.
Antiviral chemistry & chemotherapy 2001;12(6):347-51.
2001: Balzarini J; De Clercq E
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: Spaepen K; Stroobants S; Dupont P; Thomas J; Vandenberghe P; Balzarini J; De Wolf-Peeters C; Mortelmans L; Verhoef G
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: Balzarini J; Haller-Meier F; De Clercq E; Meier C
Antiviral activity of cyclosaligenyl prodrugs of acyclovir, carbovir and abacavir.
Antiviral chemistry & chemotherapy 2001;12(5):301-6.
2001: Harris S A; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
Synthesis and antiviral evaluation of phosphoramidate derivatives of (E)-5-(2-bromovinyl)-2'-deoxyuridine.
Antiviral chemistry & chemotherapy 2001;12(5):293-300.
2001: Wirsching J; Voss J; Adiwidjaja G; Balzarini J; De Clercq E
Thiosugars. VIII. Preparation of new 4'-thio-L-lyxo pyrimidine nucleoside analogues.
Nucleosides, nucleotides & nucleic acids 2001;20(9):1625-45.
2001: Brancale A; McGuigan C; Algain B; Savy P; Benhida R; Fourrey J L; Andrei G; Snoeck R; De Clercq E; Balzarini J
Bicyclic anti-VZV nucleosides: Thieno analogues retain full antiviral activity.
Bioorganic & medicinal chemistry letters 2001;11(18):2507-10.
2001: Damian F; Blaton N; Desseyn H; Clou K; Augustijns P; Naesens L; Balzarini J; Kinget R; Van den Mooter G
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: Pelemans H; Esnouf R; Min K L; Parniak M; De Clercq E; Balzarini J
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: Baraldi P G; Balboni G; Pavani M G; Spalluto G; Tabrizi M A; Clercq E D; Balzarini J; Bando T; Sugiyama H; Romagnoli R
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: Chaouni-Benabdallah A; Galtier C; Allouchi H; Kherbeche A; Debouzy J C; Teulade J C; Chavignon O; Witvrouw M; Pannecouque C; Balzarini J; de Clercq E; Enguehard C; Gueiffier A
Synthesis of 3-nitrosoimidazo[1,2-a]pyridine derivatives as potential antiretroviral agents.
Archiv der Pharmazie 2001;334(7):224-8.
2001: Barreca M L; Chimirri A; De Luca L; Monforte A M; Monforte P; Rao A; Zappalà M; Balzarini J; De Clercq E; Pannecouque C; Witvrouw M
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: Balzarini J; Camarasa M J; Pérez-Pérez M J; San-Félix A; Velázquez S; Perno C F; De Clercq E; Anderson J N; Karlsson A
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: Chamorro C; Pérez-Pérez M J; Rodríguez-Barrios F; Gago F; De Clercq E; Balzarini J; San-Félix A; Camarasa M J
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: Rodríguez-Barrios F; Pérez C; Lobatón E; Velázquez S; Chamorro C; San-Félix A; Pérez-Pérez M J; Camarasa M J; Pelemans H; Balzarini J; Gago F
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: Carangio A; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Chimirri A; Monforte P; Rao A; Zappalà M; Monforte A M; De Sarro G; Pannecouque C; Witvrouw M; Balzarini J; De Clercq E
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: Manfredini S; Baraldi P G; Durini E; Porcu L; Angusti A; Vertuani S; Solaroli N; De Clercq E; Karlsson A; Balzarini J
Design, synthesis and enzymatic activity of highly selective human mitochondrial thymidine kinase inhibitors.
Bioorganic & medicinal chemistry letters 2001;11(10):1329-32.
2001: Renze J; Plath M; Ducho C; Balzarini J; De Clercq E; Meier C
Benzyl-functionalized cycloSal-d4T monophosphates.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):931-4.
2001: Srinivasan S; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Huntley C M; Cotterill A S; Maillard J Y; Balzarini J; Simons C
Synthesis and biological evaluation of pyridin-2-one nucleosides.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):731-3.
2001: Lobatón E; Velázquez S; San-Félix A; De Clercq E; Balzarini J; Camarasa M J
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: Lobatón E; Velázquez S; Pérez-Pérez M J; Jimeno M L; San-Félix A; De Clercq E; Balzarini J; Camarasa M J
"Second generation" of TSAO compounds directed against HIV-1 TSAO-resistant strains.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):707-10.
2001: Carangio A; McGuigan C; Cahard D; Andrei G; Snoeck R; De Clercq E; Balzarini J
Synthesis and in vitro evaluation of novel anti-varicella-zoster virus (VZV) nucleosides.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):653-6.
2001: McGuigan C; Barucki H; Carangio A; Blewett S; Srinivasan S; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: De Clercq E; Andrei G; Snoeck R; De Bolle L; Naesens L; Degrève B; Balzarini J; Zhang Y; Schols D; Leyssen P; Ying C; Neyts J
Acyclic/carbocyclic guanosine analogues as anti-herpesvirus agents.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):271-85.
2001: Caamaño O; Figueira M J; Fernández F; García M D; Nieto M I; De Clercq E; Balzarini J
Synthesis and evaluation of antiviral activity of higher homologues of xylo-carbocyclic nucleosides.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):1137-9.
2001: Blewett S; McGuigan C; Barucki H; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Ballatore C; McGuigan C; De Clercq E; Balzarini J
Synthesis and evaluation of novel amidate prodrugs of PMEA and PMPA.
Bioorganic & medicinal chemistry letters 2001;11(8):1053-6.
2001: Wirsching J; Voss J; Adiwidjaja G; Balzarini J; De Clercq E
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: McGuigan C; Brancale A; Barucki H; Srinivasan S; Jones G; Pathirana R; Carangio A; Blewett S; Luoni G; Bidet O; Jukes A; Jarvis C; Andrei G; Snoeck R; De Clercq E; Balzarini J
Furano pyrimidines as novel potent and selective anti-VZV agents.
Antiviral chemistry & chemotherapy 2001;12(2):77-89.
2001: Das S R; Schneller S W; Balzarini J; De Clercq E
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: Van Laethem K; Witvrouw M; Pannecouque C; Van Remoortel B; Schmit J C; Esnouf R; Kleim J P; Balzarini J; Desmyter J; De Clercq E; Vandamme A M
Mutations in the non-nucleoside binding-pocket interfere with the multi-nucleoside resistance phenotype.
AIDS (London, England) 2001;15(5):553-61.
2001: Srinivasan S; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Dimmock J R; Padmanilayam M P; Puthucode R N; Nazarali A J; Motaganahalli N L; Zello G A; Quail J W; Oloo E O; Kraatz H B; Prisciak J S; Allen T M; Santos C L; Balzarini J; De Clercq E; Manavathu E K
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: Pelemans H; Aertsen A; Van Laethem K; Vandamme A M; De Clercq E; Pérez-Pérez M J; San-Félix A; Velázquez S; Camarasa M J; Balzarini J
Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138.
Virology 2001;280(1):97-106.
2001: Wang Z X; Duan W; Wiebe L I; Balzarini J; De Clercq E; Knaus E E
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: Wang Z X; Duan W; Wiebe L I; Balzarini J; De Clercq E; Knaus E E
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.
2001: Spaepen K; Stroobants S; Dupont P; Van Steenweghen S; Thomas J; Vandenberghe P; Vanuytsel L; Bormans G; Balzarini J; De Wolf-Peeters C; Mortelmans L; Verhoef G
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: Garoufis A; Karidi K; Hadjiliadis N; Kasselouri S; Kobe J; Balzarini J; De Clercq E
Synthesis, Characterization and Antiviral Properties of Pd(II) Complexes With Penciclovir.
Metal-based drugs 2001;8(1):57-63.
2001: Mavel S; Renou J L; Galtier C; Snoeck R; Andrei G; Balzarini J; De Clercq E; Gueiffier A
Synthesis of imidazo[1,2-a]pyridine derivatives as antiviral agents.
Arzneimittel-Forschung 2001;51(4):304-9.
2000: McGuigan C; Barucki H; Carangio A; Blewett S; Andrei G; Snoeck R; De Clercq E; Balzarini J; Erichsen J T
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: Wang Z X; Wiebe L I; Balzarini J; De Clercq E; Knaus E E
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: Raic-Malic S; Svedruzic D; Gazivoda T; Marunovic A; Hergold-Brundic A; Nagl A; Balzarini J; De Clercq E; Mintas M
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: Brancale A; Srinivasan S; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Dimmock J R; Kumar P; Nazarali A J; Motaganahalli N L; Kowalchuk T P; Beazely M A; Wilson Quail J; Oloo E O; Allen T M; Szydlowski J; DeClercq E; Balzarini J
Cytotoxic 2,6-bis(arylidene)cyclohexanones and related compounds.
European journal of medicinal chemistry 2000;35(11):967-77.
2000: Balzarini J; Aquaro S; Knispel T; Rampazzo C; Bianchi V; Perno C F; De Clercq E; Meier C
Cyclosaligenyl-2',3'-didehydro-2',3'-dideoxythymidine monophosphate: efficient intracellular delivery of d4TMP.
Molecular pharmacology 2000;58(5):928-35.
2000: Dimmock J R; Kandepu N M; Nazarali A J; Motaganahalli N L; Kowalchuk T P; Pugazhenthi U; Prisciak J S; Quail J W; Allen T M; LeClerc R; Santos C L; De Clercq E; Balzarini J
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: Balzarini J; Degrève B; Esteban-Gamboa A; Esnouf R; De Clercq E; Engelborghs Y; Camarasa M J; Pérez-Pérez M J
Kinetic analysis of novel multisubstrate analogue inhibitors of thymidine phosphorylase.
FEBS letters 2000;483(2-3):181-5.
2000: Balzarini J; Zhu C; De Clercq E; Pérez-Pérez M J; Chamorro C; Camarasa M J; Karlsson A
Novel ribofuranosylnucleoside lead compounds for potent and selective inhibitors of mitochondrial thymidine kinase-2.
The Biochemical journal 2000;351(Pt 1):167-71.
2000: McGuigan C; Pathirana R N; Jones G; Andrei G; Snoeck R; De Clercq E; Balzarini J
Anti-varicella-zoster virus bicyclic nucleosides: replacement of furo by pyrro base reduces antiviral potency.
Antiviral chemistry & chemotherapy 2000;11(5):343-8.
2000: Wang Z X; Duan W; Wiebe L I; De Clercq E; Balzarini J; Knaus E E
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: Knaggs M H; McGuigan C; Harris S A; Heshmati P; Cahard D; Gilbert I H; Balzarini J
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: Balzarini J
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: Martinez A; Gil C; Perez C; Castro A; Prieto C; Otero J; Andrei G; Snoeck R; Balzarini J; De Clercq E
Nonnucleoside human cytomegalovirus inhibitors: synthesis and antiviral evaluation of (chlorophenylmethyl)benzothiadiazine dioxide derivatives.
Journal of medicinal chemistry 2000;43(17):3267-73.
2000: Wirsching J; Voss J; Balzarini J; De Clercq E
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: Van Laethem K; Schmit J C; Pelemans H; Balzarini J; Witvrouw M; Pérez-Pérez M J; Camarasa M J; Esnouf R M; Aquaro S; Cenci A; Perno C F; Hermans P; Sprecher S; Ruiz L; Clotet B; Van Wijngaerden E; Van Ranst M; Desmyter J; De Clercq E; Vandamme A M
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: Brancale A; McGuigan C; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Wijnholds J; Mol C A; van Deemter L; de Haas M; Scheffer G L; Baas F; Beijnen J H; Scheper R J; Hatse S; De Clercq E; Balzarini J; Borst P
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: Pelemans H; Esnouf R; De Clercq E; Balzarini J
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: Tronchet J M; Kovacs I; Seman M; Dilda P; De Clercq E; Balzarini J
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: Balzarini J; De Clercq E; Carbonez A; Burt V; Kleim J P
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: Balzarini J; Degrève B; Hatse S; De Clercq E; Breuer M; Johansson M; Huybrechts R; Karlsson A
The multifunctional deoxynucleoside kinase of insect cells is a target for the development of new insecticides.
Molecular pharmacology 2000;57(4):811-9.
2000: McGuigan C; Bidois L; Hiouni A; Ballatore C; De Clercq E; Balzarini J
Phosphoramidate derivatives of stavudine as inhibitors of HIV: unnatural amino acids may substitute for alanine.
Antiviral chemistry & chemotherapy 2000;11(2):111-6.
2000: Van Laethem K; Witvrouw M; Balzarini J; Schmit J C; Sprecher S; Hermans P; Leal M; Harrer T; Ruiz L; Clotet B; Van Ranst M; Desmyter J; De Clercq E; Vandamme A M
Patient HIV-1 strains carrying the multiple nucleoside resistance mutations are cross-resistant to abacavir.
AIDS (London, England) 2000;14(4):469-71.
2000: Esteban-Gamboa A; Balzarini J; Esnouf R; De Clercq E; Camarasa M J; Pérez-Pérez M J
Design, synthesis, and enzymatic evaluation of multisubstrate analogue inhibitors of Escherichia coli thymidine phosphorylase.
Journal of medicinal chemistry 2000;43(5):971-83.
2000: Siddiqui A; McGuigan C; Ballatore C; Srinivasan S; De Clercq E; Balzarini J
Enhancing the aqueous solubility of d4T-based phosphoramidate prodrugs.
Bioorganic & medicinal chemistry letters 2000;10(4):381-4.
2000: Ren J; Diprose J; Warren J; Esnouf R M; Bird L E; Ikemizu S; Slater M; Milton J; Balzarini J; Stuart D I; Stammers D K
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: Chamorro C; De Clercq E; Balzarini J; Camarasa M J; San-Félix A
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: Aquaro S; Wedgwood O; Yarnold C; Cahard D; Pathinara R; McGuigan C; Calio' R; de Clercq E; Balzarini J; Perno C F
Activities of masked 2',3'-dideoxynucleoside monophosphate derivatives against human immunodeficiency virus in resting macrophages.
Antimicrobial agents and chemotherapy 2000;44(1):173-7.
2000: Damian F; Blaton N; Naesens L; Balzarini J; Kinget R; Augustijns P; Van den Mooter G
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.
1999: Arranz M E; Díaz J A; Ingate S T; Witvrouw M; Pannecouque C; Balzarini J; De Clercq E; Vega S
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: Velázquez S; Tuñón V; Jimeno M L; Chamorro C; De Clercq E; Balzarini J; Camarasa M J
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: Balzarini J; Naesens L; Aquaro S; Knispel T; Perno C; De Clercq E; Meier C
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: McGuigan C; Yarnold C J; Jones G; Velázquez S; Barucki H; Brancale A; Andrei G; Snoeck R; De Clercq E; Balzarini J
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: Isabel Nieto M; Manuel Blanco J; Caamaño O; Fernández F; García-Mera X; López C; Balzarini J; De Clercq E
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: Degrève B; Esnouf R; De Clercq E; Balzarini J
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: Wera S; Degrève B; Balzarini J; De Clercq E; Thevelein J M; Neyts J
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: Siddiqui A Q; McGuigan C; Ballatore C; Zuccotto F; Gilbert I H; De Clercq E; Balzarini J
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: Saboulard D; Naesens L; Cahard D; Salgado A; Pathirana R; Velazquez S; McGuigan C; De Clercq E; Balzarini J
Characterization of the activation pathway of phosphoramidate triester prodrugs of stavudine and zidovudine.
Molecular pharmacology 1999;56(4):693-704.
1999: Inguaggiato G; Hughes D; De Clercq E; Balzarini J; Simons C
Novel 6-azapyrimidine-2'-deoxy-4'-thionucleosides: synthesis, biological evaluation and conformational analysis.
Antiviral chemistry & chemotherapy 1999;10(5):241-9.
1999: Blanco J M; Caamaño O; Fernández F; García-Mera X; Hergueta A R; López C; Rodríguez-borges J E; Balzarini J; De Clercq E
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: Siddiqui A Q; McGuigan C; Ballatore C; Wedgwood O; De Clercq E; Balzarini J
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: Martínez A; Esteban A I; Herrero A; Ochoa C; Andrei G; Snoeck R; Balzarini J; De Clercq E
Imidazothiadiazine dioxides: synthesis and antiviral activity.
Bioorganic & medicinal chemistry 1999;7(8):1617-23.
1999: Manfredini S; Baraldi P G; Durini E; Vertuani S; Balzarini J; De Clercq E; Karlsson A; Buzzoni V; Thelander L
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: Hatse S; De Clercq E; Balzarini J
Role of antimetabolites of purine and pyrimidine nucleotide metabolism in tumor cell differentiation.
Biochemical pharmacology 1999;58(4):539-55.
1999: Chimirri A; Grasso S; Monforte P; Rao A; Zappalà M; Monforte A M; Pannecouque C; Witvrouw M; Balzarini J; De Clercq E
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: Hatse S; Naesens L; De Clercq E; Balzarini J
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: Balzarini J
Suppression of resistance to drugs targeted to human immunodeficiency virus reverse transcriptase by combination therapy.
Biochemical pharmacology 1999;58(1):1-27.
1999: Breistøl K; Balzarini J; Sandvold M L; Myhren F; Martinsen M; De Clercq E; Fodstad O
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: Holý A; Günter J; Dvoráková H; Masojídková M; Andrei G; Snoeck R; Balzarini J; De Clercq E
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: Velázquez S; Tuñón V; Jimeno M L; Pérez-Pérez M J; San-Félix A; Chamorro C; Lobatón E; Esteban-Gamboa A; De Clercq E; Balzarini J; Camarasa M J
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: Manfredini S; Baraldi P G; Durini E; Balzarini J; De Clercq E; Karlsson A; Buzzoni V; Thelander L
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: Bazzanini R; Manfredini S; Durini E; Gröschel B; Cinatl J; Balzarini J; De Clercq E; Imbach J L; Périgaud C; Gosselin G
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: Ballatore C; McGuigan C; De Clercq E; Balzarini J
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: Meier C; Knispel T; Marquez V E; De Clercq E; Balzarini J
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: De Clercq E; Andrei G; Balzarini J; Hatse S; Liekens S; Naesens L; Neyts J; Snoeck R
Antitumor potential of acyclic nucleoside phosphonates.
Nucleosides & nucleotides 1999;18(4-5):759-71.
1999: Santana L; Teijeira M; Uriarte E; Terán C; Andrei G; Snoeck R; Balzarini J; De Clercq E
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: Lobatón E; Velázquez S; San-Félix A; Chamorro C; Tuñón V; Esteban-Gamboa A; De Clercq E; Balzarini J; Camarasa M J; Pérez-Pérez M J
Novel TSAO derivatives modified at positions 3" and 4" of the spiro moiety.
Nucleosides & nucleotides 1999;18(4-5):675-6.
1999: Nieto I; Figueira M J; Blanco J M; Caamaño O; Fernández F; De Clercq E; Balzarini J
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: Dimmock J R; Kandepu N M; Nazarali A J; Kowalchuk T P; Motaganahalli N; Quail J W; Mykytiuk P A; Audette G F; Prasad L; Perjési P; Allen T M; Santos C L; Szydlowski J; De Clercq E; Balzarini J
Conformational and quantitative structure-activity relationship study of cytotoxic 2-arylidenebenzocycloalkanones.
Journal of medicinal chemistry 1999;42(8):1358-66.
1999: Martinez A; Esteban A I; Castro A; Gil C; Conde S; Andrei G; Snoeck R; Balzarini J; De Clercq E
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: Kleim J P; Winters M; Dunkler A; Suarez J R; Riess G; Winkler I; Balzarini J; Oette D; Merigan T C
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: Hatse S; De Clercq E; Balzarini J
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: Siddiqui A Q; Ballatore C; McGuigan C; De Clercq E; Balzarini J
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: Naesens L; Hatse S; Segers C; Verbeken E; De Clercq E; Waer M; Balzarini J
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: Pelemans H; Esnouf R M; Jonckheere H; De Clercq E; Balzarini J
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: Gueiffier A; Mavel S; Lhassani M; Elhakmaoui A; Snoeck R; Andrei G; Chavignon O; Teulade J C; Witvrouw M; Balzarini J; De Clercq E; Chapat J P
Synthesis of imidazo[1,2-a]pyridines as antiviral agents.
Journal of medicinal chemistry 1998;41(25):5108-12.
1998: Degrève B; Johansson M; De Clercq E; Karlsson A; Balzarini J
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: McGuigan C; Cahard D; Ballatore C; Siddiqui A; De Clercq E; Balzarini J
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: Velázquez S; Alvarez R; Pérez C; Gago F; De Clercq E; Balzarini J; Camarasa M J
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: McGuigan C; Sutton P W; Cahard D; Turner K; O'Leary G; Wang Y; Gumbleton M; De Clercq E; Balzarini J
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: Van den Mooter G; Stas G; Damian F; Naesens L; Balzarini J; Kinget R; Augustijns P
Stability of UC-781, in intestinal mucosal homogenates of the rat, rabbit, and pig.
Pharmaceutical research 1998;15(11):1799-802.
1998: Velázquez S; Chamorro C; Pérez-Pérez M J; Alvarez R; Jimeno M L; Martín-Domenech A; Pérez C; Gago F; De Clercq E; Balzarini J; San-Félix A; Camarasa M J
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: Hatse S; De Clercq E; Balzarini J
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: Balzarini J; Gamboa A E; Esnouf R; Liekens S; Neyts J; De Clercq E; Camarasa M J; Pérez-Pérez M J
7-Deazaxanthine, a novel prototype inhibitor of thymidine phosphorylase.
FEBS letters 1998;438(1-2):91-5.
1998: Hatse S; Naesens L; De Clercq E; Balzarini J
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: Arranz E; Díaz J A; Ingate S T; Witvrouw M; Pannecouque C; Balzarini J; De Clercq E; Vega S
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: Dimmock J R; Vashishtha S C; Quail J W; Pugazhenthi U; Zimpel Z; Sudom A M; Allen T M; Kao G Y; Balzarini J; De Clercq E
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: Chamorro C; Camarasa M J; Pérez-Pérez M J; de Clercq E; Balzarini J; San Félix A
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: Witvrouw M; Daelemans D; Pannecouque C; Neyts J; Andrei G; Snoeck R; Vandamme A M; Balzarini J; Desmyter J; Baba M; De Clercq E
Broad-spectrum antiviral activity and mechanism of antiviral action of the fluoroquinolone derivative K-12.
Antiviral chemistry & chemotherapy 1998;9(5):403-11.
1998: Robins M J; Wnuk S F; Yang X; Yuan C S; Borchardt R T; Balzarini J; De Clercq E
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: Alvarez R; Jimeno M L; Gago F; Balzarini J; Pérez-Pérez M J; Camarasa M J
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: Nieto M I; Blanco J M; Caamaño O; Fernández F; García-Mera X; Balzarini J; Padalko E; Neyts J; De Clercq E
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: Borges J E; Fernández F; García X; Hergueta A R; López C; Andrei G; Snoeck R; Witvrounw M; Balzarini J; De Clercq E
Novel carbocyclic nucleosides containing a cyclobutyl ring. Guanosine and adenosine analogues.
Nucleosides & nucleotides 1998;17(7):1237-53.
1998: Wnuk S F; Mao Y; Yuan C S; Borchardt R T; Andrei G; Balzarini J; De Clercq E; Robins M J
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: Balzarini J; Naesens L; Verbeken E; Laga M; Van Damme L; Parniak M; Van Mellaert L; Anné J; De Clercq E
Preclinical studies on thiocarboxanilide UC-781 as a virucidal agent.
AIDS (London, England) 1998;12(10):1129-38.
1998: Santana L; Teijeira M; Uriarte E; Balzarini J; De Clercq E
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: Pelemans H; Esnouf R M; Parniak M A; Vandamme A M; De Clercq E; Balzarini J
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: Goldring A O; Balzarini J; Gilbert I H
Design and synthesis of bio-isosteres of thymidine triphosphate.
Bioorganic & medicinal chemistry letters 1998;8(10):1211-4.
1998: Ochoa C; Provencio R; Jimeno M L; Balzarini J; De Clercq E
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: Hatse S; Naesens L; Degrève B; Segers C; Vandeputte M; Waer M; De Clercq E; Balzarini J
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: Balzarini J; Cahard D; Wedgwood O; Salgado A; Velázquez S; Yarnold C J; De Clercq E; McGuigan C; Thormar H
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: McGuigan C; Tsang H W; Sutton P W; De Clercq E; Balzarini J
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: Balzarini J; Degrève B; Andrei G; Neyts J; Sandvold M; Myhren F; de Clercq E
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: Balzarini J; Hatse S; Naesens L; De Clercq E
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: Dimmock J R; Kandepu N M; Hetherington M; Quail J W; Pugazhenthi U; Sudom A M; Chamankhah M; Rose P; Pass E; Allen T M; Halleran S; Szydlowski J; Mutus B; Tannous M; Manavathu E K; Myers T G; De Clercq E; Balzarini J
Cytotoxic activities of Mannich bases of chalcones and related compounds.
Journal of medicinal chemistry 1998;41(7):1014-26.
1998: Witvrouw M; Arranz M E; Pannecouque C; Declercq R; Jonckheere H; Schmit J C; Vandamme A M; Diaz J A; Ingate S T; Desmyter J; Esnouf R; Van Meervelt L; Vega S; Balzarini J; De Clercq E
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: Balzarini J; Pelemans H; Riess G; Roesner M; Winkler I; De Clercq E; Kleim J P
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: Balzarini J; Pelemans H; Esnouf R; De Clercq E
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: Hartmann K; Kuffer M; Balzarini J; Naesens L; Goldberg M; Erfle V; Goebel F D; De Clercq E; Jindrich J; Holy A; Bischofberger N; Kraft W
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: Neyts J; Balzarini J; Andrei G; Chaoyong Z; Snoeck R; Zimmermann A; Mertens T; Karlsson A; De Clercq E
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.
1998: Naesens L; Cahard D; Salgado A; Bidois L; De Clercq E; McGuigan C; Balzarini J
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: Balzarini J; Stet L; Matsuda A; Wiebe L; Knauss E; De Clercq E
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: Hatse S; Naesens L; Degrève B; Vandeputte M; Waer M; De Clercq E; Balzarini J
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.
1997: Kuffer M; Balzarini J; Rolinski B; Goebel F; Erfle V; Goldberg M; Hartmann K
[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: Manfredini S; Simoni D; Ferroni R; Bazzanini R; Vertuani S; Hatse S; Balzarini J; De Clercq E
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: Balzarini J; Pelemans H; Riess G; Roesner M; Winkler I; De Clercq E; Kleim J P
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: Pelemans H; Esnouf R; Dunkler A; Parniak M A; Vandamme A M; Karlsson A; De Clercq E; Kleim J P; Balzarini J
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: Degrève B; Andrei G; Izquierdo M; Piette J; Morin K; Knaus E E; Wiebe L I; Basrah I; Walker R T; De Clercq E; Balzarini J
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: De Groote K; Naesens L; Balzarini J; Baes M I; Declercq P E
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: Balo C; Fernández F; Lens E; López C; Andrei G; Snoeck R; Balzarini J; De CLercq E
Novel carbocyclic nucleosides containing a cyclopentyl ring. Adenosine and uridine analogues.
Archiv der Pharmazie 1997;330(8):265-7.
1997: McGuigan C; Tsang H W; Cahard D; Turner K; Velazquez S; Salgado A; Bidois L; Naesens L; De Clercq E; Balzarini J
Phosphoramidate derivatives of d4T as inhibitors of HIV: the effect of amino acid variation.
Antiviral research 1997;35(3):195-204.
1997: Aquaro S; Perno C F; Balestra E; Balzarini J; Cenci A; Francesconi M; Panti S; Serra F; Villani N; Caliò R
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: Balzarini J; Kruining J; Wedgwood O; Pannecouque C; Aquaro S; Perno C F; Naesens L; Witvrouw M; Heijtink R; De Clercq E; McGuigan C
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: Balzarini J; De Clercq E; Uberla K
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: Esnouf R M; Stuart D I; De Clercq E; Schwartz E; Balzarini J
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: Wnuk S F; Yuan C S; Borchardt R T; Balzarini J; De Clercq E; Robins M J
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: Dimmock J R; Kumar P; Allen T M; Kao G Y; Halleran S; Balzarini J; de Clercq E
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: Balzarini J; Vahlenkamp T; Egberink H; Hartmann K; Witvrouw M; Pannecouque C; Casara P; Navé J F; De Clercq E
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: Perno C F; Santoro N; Balestra E; Aquaro S; Cenci A; Lazzarino G; Di Pierro D; Tavazzi B; Balzarini J; Garaci E; Grimaldi S; Caliò R
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: Witvrouw M; Balzarini J; Pannecouque C; Jhaumeer-Laulloo S; Esté J A; Schols D; Cherepanov P; Schmit J C; Debyser Z; Vandamme A M; Desmyter J; Ramadas S R; de Clercq E
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: Balzarini J; Pelemans H; De Clercq E; Karlsson A; Kleim J P
Reverse transcriptase fidelity and HIV-1 variation.
Science (New York, N.Y.) 1997;275(5297):229-30; author reply 230-1.
1996: Ingate S; De Clercq E; Balzarini J; Camarasa M J
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: Balzarini J; Pelemans H; Karlsson A; De ClercQ E; Kleim J P
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: Hatse S; De Clercq E; Balzarini J
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: Balzarini J; Egberink H; Hartmann K; Cahard D; Vahlenkamp T; Thormar H; De Clercq E; McGuigan C
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: Schmit J C; Cogniaux J; Hermans P; Van Vaeck C; Sprecher S; Van Remoortel B; Witvrouw M; Balzarini J; Desmyter J; De Clercq E; Vandamme A M
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: Jonckheere H; De Vreese K; Debyser Z; Vandekerckhove J; Balzarini J; Desmyter J; De Clercq E; Anné J
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: Holý A; Dvoráková H; Jindrich J; Masojídková M; Budesínský M; Balzarini J; Andrei G; De Clercq E
Acyclic nucleotide analogs derived from 8-azapurines: synthesis and antiviral activity.
Journal of medicinal chemistry 1996;39(20):4073-88.
1996: Obara T; Shuto S; Saito Y; Snoeck R; Andrei G; Balzarini J; De Clercq E; Matsuda A
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: Tsotinis A; Calogeropoulou T; Koufaki M; Souli C; Balzarini J; De Clercq E; Makriyannis A
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: Kolocouris N; Kolocouris A; Foscolos G B; Fytas G; Neyts J; Padalko E; Balzarini J; Snoeck R; Andrei G; De Clercq E
Synthesis and antiviral activity evaluation of some new aminoadamantane derivatives. 2.
Journal of medicinal chemistry 1996;39(17):3307-18.
1996: Dvoráková H; Masojídková M; Holý A; Balzarini J; Andrei G; Snoeck R; De Clercq E
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: Balzarini J; Wedgwood O; Kruining J; Pelemans H; Heijtink R; De Clercq E; McGuigan C
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: Balzarini J; Pelemans H; Aquaro S; Perno C F; Witvrouw M; Schols D; De Clercq E; Karlsson A
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: Perno C F; Balestra E; Aquaro S; Panti S; Cenci A; Lazzarino G; Tavazzi B; Di Pierro D; Balzarini J; Calio R
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: Balzarini J; Karlsson A; Aquaro S; Perno C F; Cahard D; Naesens L; De Clercq E; McGuigan C
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: Van Damme E J; Barre A; Rougé P; Van Leuven F; Balzarini J; Peumans W J
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: Balzarini J; Brouwer W G; Dao D C; Osika E M; De Clercq E
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: Balzarini J; Pelemans H; Pérez-Pérez M J; San-Félix A; Camarasa M J; De Clercq E; Karlsson A
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: McGuigan C; Cahard D; Sheeka H M; De Clercq E; Balzarini J
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: Balzarini J; Aquaro S; Perno C F; Witvrouw M; Holý A; De Clercq E
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: Naesens L; Balzarini J; Bischofberger N; De Clercq E
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.
1996: Balzarini J; De Clercq E
Analysis of inhibition of retroviral reverse transcriptase.
Methods in enzymology 1996;275():472-502.
1995: Reymen D; Naesens L; Balzarini J; Holý A; Dvoráková H; De Clercq E
Antiviral activity of selected acyclic nucleoside analogues against human herpesvirus 6.
Antiviral research 1995;28(4):343-57.
1995: Balzarini J; Andrei G; Kumar R; Knaus E E; Wiebe L I; De Clercq E
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: Balzarini J; Morin K W; Knaus E E; Wiebe L I; De Clercq E
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: Ingate S; Pérez-Pérez M J; De Clercq E; Balzarini J; Camarasa M J
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: Balzarini J; Brouwer W G; Felauer E E; De Clercq E; Karlsson A
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: Balzarini J; Weeger M; Camarasa M J; De Clercq E; Uberla K
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: Balzarini J; Pérez-Pérez M J; Vélazquez S; San-Félix A; Camarasa M J; De Clercq E; Karlsson A
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: Velázquez S; Alvarez R; San-Félix A; Jimeno M L; De Clercq E; Balzarini J; Camarasa M J
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: Thormar H; Balzarini J; Debyser Z; Witvrouw M; Desmyter J; De Clercq E
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: Thormar H; Georgsson G; Pálsson P A; Balzarini J; Naesens L; Torsteinsdóttir S; De Clercq E
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: Balzarini J; Baba M; De Clercq E
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: Verheggen I; Van Aerschot A; Van Meervelt L; Rozenski J; Wiebe L; Snoeck R; Andrei G; Balzarini J; Claes P; De Clercq E
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: Balzarini J; Verstuyf A; Hatse S; Goebels J; Sobis H; Vandeputte M; De Clercq E
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: Manfredini S; Baraldi P G; Bazzanini R; Marangoni M; Simoni D; Balzarini J; De Clercq E
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: Naesens L; Balzarini J; De Clercq E
The potential of acyclic nucleoside phosphonates as broad-spectrum antiviral agents.
Postepy biochemii 1995;41(5 Suppl):347-51.
1995: Balzarini J
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: Neyts J; Andrei G; Snoeck R; Jähne G; Winkler I; Helsberg M; Balzarini J; De Clercq E
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: Balzarini J; Karlsson A; Meichsner C; Paessens A; Riess G; De Clercq E; Kleim J P
Resistance pattern of human immunodeficiency virus type 1 reverse transcriptase to quinoxaline S-2720.
Journal of virology 1994;68(12):7986-92.
1994: Alvarez R; Velázquez S; San-Félix A; Aquaro S; De Clercq E; Perno C F; Karlsson A; Balzarini J; Camarasa M J
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: Wnuk S F; Yuan C S; Borchardt R T; Balzarini J; De Clercq E; Robins M J
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: Villani N; Caliò R; Balestra E; Balzarini J; De Clercq E; Fabrizi E; Perno C F; Del Gobbo V
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: Jonckheere H; Taymans J M; Balzarini J; Velázquez S; Camarasa M J; Desmyter J; De Clercq E; Anné J
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: Van Damme E J; Balzarini J; Smeets K; Van Leuven F; Peumans W J
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: Manfredini S; Baraldi P G; Bazzanini R; Guarneri M; Simoni D; Balzarini J; De Clercq E
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: Balzarini J; Karlsson A; Sardana V V; Emini E A; Camarasa M J; De Clercq E
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: Balzarini J; Bohman C; Walker R T; de Clercq E
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: Balzarini J; Kleim J P; Riess G; Camarasa M J; De Clercq E; Karlsson A
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: Snoeck R; Gérard M; Sadzot-Delvaux C; Andrei G; Balzarini J; Reymen D; Ahadi N; De Bruyn J M; Piette J; Rentier B
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: Snoeck R; Andrei G; Gérard M; Silverman A; Hedderman A; Balzarini J; Sadzot-Delvaux C; Tricot G; Clumeck N; De Clercq E
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: Balzarini J
Metabolism and mechanism of antiretroviral action of purine and pyrimidine derivatives.
Pharmacy world & science : PWS 1994;16(2):113-26.
1994: De Clercq E; Yamamoto N; Pauwels R; Balzarini J; Witvrouw M; De Vreese K; Debyser Z; Rosenwirth B; Peichl P; Datema R
Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM3100.
Antimicrobial agents and chemotherapy 1994;38(4):668-74.
1994: Bohman C; Balzarini J; Wigerinck P; Van Aerschot A; Herdewijn P; De Clercq E
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: San-Félix A; Velázquez S; Pérez-Pérez M J; Balzarini J; De Clercq E; Camarasa M J
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: Caliò R; Villani N; Balestra E; Sesa F; Holy A; Balzarini J; De Clercq E; Perno C F; Del Gobbo V
Enhancement of natural killer activity and interferon induction by different acyclic nucleoside phosphonates.
Antiviral research 1994;23(1):77-89.
1993: Thormar H; Balzarini J; Holy A; Jindrich J; Rosenberg I; Debyser Z; Desmyter J; De Clercq E
Inhibition of visna virus replication by 2',3'-dideoxynucleosides and acyclic nucleoside phosphonate analogs.
Antimicrobial agents and chemotherapy 1993;37(12):2540-4.
1993: Snoeck R; Gérard M; Sadzot-Delvaux C; Andrei G; Balzarini J; Reymen D; Piette J; Rentier B; Clumeck N; De Clercq E
Meningoradiculoneuritis due to acyclovir-resistant varicella-zoster virus in a patient with AIDS.
The Journal of infectious diseases 1993;168(5):1330-1.
1993: Balzarini J; Karlsson A; Wang L; Bohman C; Horská K; Votruba I; Fridland A; Van Aerschot A; Herdewijn P; De Clercq E
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: Velázquez S; San-Félix A; Pérez-Pérez M J; Balzarini J; De Clercq E; Camarasa M J
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: Van Damme E J; Smeets K; Engelborghs I; Aelbers H; Balzarini J; Pusztai A; van Leuven F; Goldstein I J; Peumans W J
Cloning and characterization of the lectin cDNA clones from onion, shallot and leek.
Plant molecular biology 1993;23(2):365-76.
1993: Pérez-Pérez M J; Balzarini J; De Clercq E; Camarasa M J
Glycosyl-oxycarbonylaminosulfonyl-2',3'-dideoxynucleoside derivatives as lipophilic nucleotide mimics. Synthesis and anti-HIV activity.
Bioorganic & medicinal chemistry 1993;1(4):279-84.
1993: Balzarini J; Karlsson A; De Clercq E
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: Balzarini J; Karlsson A; Pérez-Pérez M J; Camarasa M J; De Clercq E
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: Balzarini J; Karlsson A; Pérez-Pérez M J; Camarasa M J; Tarpley W G; De Clercq E
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: Papadaki-Valiraki A; Papakonstantinou-Garoufalias S; Marakos P; Chytyroglou-Lada A; Hosoya M; Balzarini J; de Clercq E
Synthesis, antifungal, antibacterial and antiviral effects of some adamantaneketoxime ethers.
Farmaco (Società chimica italiana : 1989) 1993;48(8):1091-102.
1993: Balzarini J; Karlsson A; Vandamme A M; Pérez-Pérez M J; Zhang H; Vrang L; Oberg B; Bäckbro K; Unge T; San-Félix A
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: Verheggen I; Van Aerschot A; Toppet S; Snoeck R; Janssen G; Balzarini J; De Clercq E; Herdewijn P
Synthesis and antiherpes virus activity of 1,5-anhydrohexitol nucleosides.
Journal of medicinal chemistry 1993;36(14):2033-40.
1993: Snoeck R; Andrei G; Neyts J; Schols D; Cools M; Balzarini J; De Clercq E
Inhibitory activity of S-adenosylhomocysteine hydrolase inhibitors against human cytomegalovirus replication.
Antiviral research 1993;21(3):197-216.
1993: Balzarini J; Naesens L; Bohman C; Pérez-Pérez M J; San-Félix A; Camarasa M J; De Clercq E
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: McGuigan C; Pathirana R N; Balzarini J; De Clercq E
Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT.
Journal of medicinal chemistry 1993;36(8):1048-52.
1993: Balzarini J; Bohman C; De Clercq E
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: Balzarini J; Holy A; Jindrich J; Naesens L; Snoeck R; Schols D; De Clercq E
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: Naesens L; Neyts J; Balzarini J; Holy A; Rosenberg I; De Clercq E
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: Balzarini J; Karlsson A; Pérez-Pérez M J; Vrang L; Walbers J; Zhang H; Oberg B; Vandamme A M; Camarasa M J; De Clercq E
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: Balzarini J; Velazquez S; San-Felix A; Karlsson A; Perez-Perez M J; Camarasa M J; De Clercq E
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: Snoeck R; Andrei G; Schols D; Balzarini J; De Clercq E
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: Yamamoto N; Schols D; De Clercq E; Debyser Z; Pauwels R; Balzarini J; Nakashima H; Baba M; Hosoya M; Snoeck R
Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents.
Molecular pharmacology 1992;42(6):1109-17.
1992: Balzarini J; De Clercq E
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: Naesens L; Balzarini J; De Clercq E
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: Bergamini A; Perno C F; Balzarini J; Capozzi M; Marinelli L; Milanese G; Pesce C D; Calió R; Rocchi G
Selective inhibition of HIV replication by adriamycin in macrophages but not in lymphocytes.
AIDS research and human retroviruses 1992;8(7):1239-47.
1992: Neyts J; Snoeck R; Schols D; Balzarini J; Esko J D; Van Schepdael A; De Clercq E
Sulfated polymers inhibit the interaction of human cytomegalovirus with cell surface heparan sulfate.
Virology 1992;189(1):48-58.
1992: Robins M J; Samano V; Zhang W; Balzarini J; De Clercq E; Borchardt R T; Lee Y; Yuan C S
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: De Clercq E; Yamamoto N; Pauwels R; Baba M; Schols D; Nakashima H; Balzarini J; Debyser Z; Murrer B A; Schwartz D
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: Balzarini J; Pérez-Pérez M J; San-Félix A; Camarasa M J; Bathurst I C; Barr P J; De Clercq E
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: Balzarini J; Neyts J; Schols D; Hosoya M; Van Damme E; Peumans W; De Clercq E
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: Baraldi P G; Manfredini S; Simoni D; Tabrizi M A; Balzarini J; De Clercq E
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: Balzarini J; Pérez-Pérez M J; San-Félix A; Velazquez S; Camarasa M J; De Clercq E
[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: Balzarini J; Pérez-Pérez M J; San-Félix A; Schols D; Perno C F; Vandamme A M; Camarasa M J; De Clercq E
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: Naesens L; Balzarini J; De Clercq E
Acyclic adenine nucleoside phosphonates in plasma determined by high-performance liquid chromatography with fluorescence detection.
Clinical chemistry 1992;38(4):480-5.
1992: Perno C F; Yarchoan R; Balzarini J; Bergamini A; Milanese G; Pauwels R; De Clercq E; Rocchi G; Calio R
Different pattern of activity of inhibitors of the human immunodeficiency virus in lymphocytes and monocyte/macrophages.
Antiviral research 1992;17(4):289-304.
1992: Shuto S; Obara T; Toriya M; Hosoya M; Snoeck R; Andrei G; Balzarini J; De Clercq E
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: Hosoya M; Balzarini J; Shigeta S; De Clercq E
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: Simoni D; Manfredini S; Tabrizi M A; Bazzanini R; Baraldi P G; Balzarini J; De Clercq E
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: Balzarini J; Lee C K; Herdewijn P; De Clercq E
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: Balzarini J; Perno C F; Schols D; De Clercq E
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: Naesens L; Balzarini J; De Clercq E
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: Del Gobbo V; Foli A; Balzarini J; De Clercq E; Balestra E; Villani N; Marini S; Perno C F; Calio R
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: Neyts J; Snoeck R; Balzarini J; De Clercq E
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: Balzarini J; Lee C K; Schols D; De Clercq E
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: Cools M; Balzarini J; De Clercq E
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: Balzarini J; Holy A; Jindrich J; Dvorakova H; Hao Z; Snoeck R; Herdewijn P; Johns D G; De Clercq E
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: Balzarini J; De Clercq E
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: De Clercq E; Cools M; Balzarini J; Snoeck R; Andrei G; Hosoya M; Shigeta S; Ueda T; Minakawa N; Matsuda A
Antiviral activities of 5-ethynyl-1-beta-D-ribofuranosylimidazole-4- carboxamide and related compounds.
Antimicrobial agents and chemotherapy 1991;35(4):679-84.
1991: Balzarini J; Schols D; Neyts J; Van Damme E; Peumans W; De Clercq E
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: Balzarini J; Hao Z; Herdewijn P; Johns D G; De Clercq E
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: Balzarini J; Naesens L; Slachmuylders J; Niphuis H; Rosenberg I; Holý A; Schellekens H; De Clercq E
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: Balzarini J; De Clercq E
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: Van Aerschot A; Everaert D; Gosselin G; Peeters O; Blaton N; De Ranter C; Imbach J L; Balzarini J; De Clercq E; Herdewijn P
2'-Azido-2',3'-dideoxythymidine: synthesis and crystal structure of a 2'-substituted dideoxynucleoside.
Antiviral research 1990;14(6):357-69.
1990: Balzarini J; De Clercq E
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: Neyts J; Snoeck R; Schols D; Balzarini J; De Clercq E
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: Jie L; Van Aerschot A; Balzarini J; Janssen G; Busson R; Hoogmartens J; De Clercq E; Herdewijn P
5'-O-phosphonomethyl-2',3'-dideoxynucleosides: synthesis and anti-HIV activity.
Journal of medicinal chemistry 1990;33(9):2481-7.
1990: Balzarini J; Naesens L; De Clercq E
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: Snoeck R; Lagneaux L; Delforge A; Bron D; Van der Auwera P; Stryckmans P; Balzarini J; De Clercq E
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: Nakashima H; Balzarini J; Pauwels R; Schols D; Desmyter J; De Clercq E
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: Van Aerschot A; Everaert D; Balzarini J; Augustyns K; Jie L; Janssen G; Peeters O; Blaton N; De Ranter C; De Clercq E
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: Balzarini J; Sobis H; Naesens L; Vandeputte M; De Clercq E
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: Balzarini J; Bernaerts R; Verbruggen A; De Clercq E
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: Balzarini J; De Clercq E; Baumgartner H; Bodenteich M; Griengl H
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: Wigerinck P; Van Aerschot A; Janssen G; Claes P; Balzarini J; De Clercq E; Herdewijn P
Synthesis and antiviral activity of 3'-heterocyclic substituted 3'-deoxythymidines.
Journal of medicinal chemistry 1990;33(2):868-73.
1990: Balzarini J; Naesens L; Robins M J; De Clercq E
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: Witvrouw M; Baba M; Balzarini J; Pauwels R; De Clercq E
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: Baba M; Tanaka H; De Clercq E; Pauwels R; Balzarini J; Schols D; Nakashima H; Perno C F; Walker R T; Miyasaka T
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: Naesens L; Balzarini J; Rosenberg I; Holý A; De Clercq E
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: Balzarini J; Van Aerschot A; Herdewijn P; De Clercq E
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: Robins M J; Wood S G; Dalley N K; Herdewijn P; Balzarini J; De Clercq E
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: Van Aerschot A; Herdewijn P; Balzarini J; Pauwels R; De Clercq E
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: De Clercq E; Cools M; Balzarini J; Marquez V E; Borcherding D R; Borchardt R T; Drach J C; Kitaoka S; Konno T
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: Balzarini J; Baumgartner H; Bodenteich M; De Clercq E; Griengl H
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: De Clercq E; Cools M; Balzarini J
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: Balzarini J; De Clercq E
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: Balzarini J; Van Aerschot A; Pauwels R; Baba M; Schols D; Herdewijn P; De Clercq E
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: Balzarini J; Herdewijn P; De Clercq E
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: Balzarini J; Herdewijn P; De Clercq E
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: Balzarini J; van Aerschot A; Herdewijn P; de Clercq E
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: Baraldi P G; Guarneri M; Manfredini S; Simoni D; Balzarini J; De Clercq E
Synthesis and cytostatic activity of geiparvarin analogues.
Journal of medicinal chemistry 1989;32(2):284-8.
1989: Balzarini J; De Clercq E
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: Balzarini J; Cools M; De Clercq E
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: Balzarini J; Naesens L; Herdewijn P; Rosenberg I; Holy A; Pauwels R; Baba M; Johns D G; De Clercq E
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: Balzarini J; Matthes E; Meeus P; Johns D G; De Clercq E
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: Schols D; Pauwels R; Vanlangendonck F; Balzarini J; De Clercq E
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: Herdewijn P; Balzarini J; Baba M; Pauwels R; Van Aerschot A; Janssen G; De Clercq E
Synthesis and anti-HIV activity of different sugar-modified pyrimidine and purine nucleosides.
Journal of medicinal chemistry 1988;31(10):2040-8.
1988: Baba M; Schols D; Pauwels R; Balzarini J; De Clercq E
Fuchsin acid selectively inhibits human immunodeficiency virus (HIV) replication in vitro.
Biochemical and biophysical research communications 1988;155(3):1404-11.
1988: Baba M; Nakajima M; Schols D; Pauwels R; Balzarini J; De Clercq E
Pentosan polysulfate, a sulfated oligosaccharide, is a potent and selective anti-HIV agent in vitro.
Antiviral research 1988;9(6):335-43.
1988: Pauwels R; Balzarini J; Baba M; Snoeck R; Schols D; Herdewijn P; Desmyter J; De Clercq E
Rapid and automated tetrazolium-based colorimetric assay for the detection of anti-HIV compounds.
Journal of virological methods 1988;20(4):309-21.
1988: Baba M; Pauwels R; Balzarini J; Arnout J; Desmyter J; De Clercq E
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: Pauwels R; Balzarini J; Schols D; Baba M; Desmyter J; Rosenberg I; Holy A; De Clercq E
Phosphonylmethoxyethyl purine derivatives, a new class of anti-human immunodeficiency virus agents.
Antimicrobial agents and chemotherapy 1988;32(7):1025-30.
1988: Balzarini J; Baba M; Pauwels R; Herdewijn P; De Clerq E
Anti-retrovirus activity of 3'-fluoro- and 3'-azido-substituted pyrimidine 2',3'-dideoxynucleoside analogues.
Biochemical pharmacology 1988;37(14):2847-56.
1988: Balzarini J; Herdewijn P; Pauwels R; Broder S; De Clercq E
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: Pauwels R; Baba M; Balzarini J; Herdewijn P; Desmyter J; Robins M J; Zou R M; Madej D; De Clercq E
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: Keizer H J; Pauwels R; Landuyt W; Balzarini J; van der Schueren E; De Clercq E
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: Balzarini J; Baba M; Pauwels R; Herdewijn P; Wood S G; Robins M J; de Clercq E
Potent and selective activity of 3'-azido-2,6-diaminopurine-2',3'-dideoxyriboside, 3'-fluoro-2,6-diaminopurine-2',3'-dideoxyriboside, and 3'-fluoro-2',3'-dideoxyguanosine against human immunodeficiency virus.
Molecular pharmacology 1988;33(3):243-9.
1988: Balzarini J; Pauwels R; Baba M; Herdewijn P; de Clercq E; Broder S; Johns D G
The in vitro and in vivo anti-retrovirus activity, and intracellular metabolism of 3'-azido-2',3'-dideoxythymidine and 2',3'-dideoxycytidine are highly dependent on the cell species.
Biochemical pharmacology 1988;37(5):897-903.
1987: De Clercq E; Sakuma T; Baba M; Pauwels R; Balzarini J; Rosenberg I; Holý A
Antiviral activity of phosphonylmethoxyalkyl derivatives of purine and pyrimidines.
Antiviral research 1987;8(5-6):261-72.
1987: Herdewijn P; Pauwels R; Baba M; Balzarini J; De Clercq E
Synthesis and anti-HIV activity of various 2'- and 3'-substituted 2',3'-dideoxyadenosines: a structure-activity analysis.
Journal of medicinal chemistry 1987;30(11):2131-7.
1987: Baba M; Pauwels R; Balzarini J; Herdewijn P; De Clercq E; Desmyter J
Ribavirin antagonizes inhibitory effects of pyrimidine 2',3'-dideoxynucleosides but enhances inhibitory effects of purine 2',3'-dideoxynucleosides on replication of human immunodeficiency virus in vitro.
Antimicrobial agents and chemotherapy 1987;31(10):1613-7.
1987: Balzarini J; De Clercq E; Verbruggen A; Ayusawa D; Shimizu K; Seno T
Thymidylate synthase is the principal target enzyme for the cytostatic activity of (E)-5-(2-bromovinyl)-2'-deoxyuridine against murine mammary carcinoma (FM3A) cells transformed with the herpes simplex virus type 1 or type 2 thymidine kinase gene.
Molecular pharmacology 1987;32(3):410-6.
1987: Pauwels R; De Clercq E; Desmyter J; Balzarini J; Goubau P; Herdewijn P; Vanderhaeghe H; Vandeputte M
Sensitive and rapid assay on MT-4 cells for detection of antiviral compounds against the AIDS virus.
Journal of virological methods 1987;16(3):171-85.
1987: Balzarini J; Robins M J; Zou R M; Herdewijn P; De Clercq E
The 2',3'-dideoxyriboside of 2,6-diaminopurine and its 2',3'-didehydro derivative inhibit the deamination of 2',3'-dideoxyadenosine, an inhibitor of human immunodeficiency virus (HIV) replication.
Biochemical and biophysical research communications 1987;145(1):277-83.
1987: Balzarini J; Pauwels R; Baba M; Robins M J; Zou R M; Herdewijn P; De Clercq E
The 2',3'-dideoxyriboside of 2,6-diaminopurine selectively inhibits human immunodeficiency virus (HIV) replication in vitro.
Biochemical and biophysical research communications 1987;145(1):269-76.
1987: Balzarini J; De Clercq E
Differential affinities of pyrimidine nucleoside analogues for deoxythymidine and deoxycytidine kinase determine their incorporation into murine leukemia L1210 cells.
Acta biochimica Polonica 1987;34(2):63-77.
1985: De Clercq E; Bernaerts R; Balzarini J; Herdewijn P; Verbruggen A
Metabolism of the carbocyclic analogue of (E)-5-(2-iodovinyl)-2'-deoxyuridine in herpes simplex virus-infected cells. Incorporation of C-IVDU into DNA.
The Journal of biological chemistry 1985;260(19):10621-8.
1985: De Clercq E; Balzarini J; Bernaerts R; Herdewijn P; Verbruggen A
Selective antiherpetic activity of carbocyclic analogues of (E)-5-(2-halogenovinyl)-2'-deoxyuridines: dependence on specific phosphorylation by viral thymidine kinase.
Biochemical and biophysical research communications 1985;126(1):397-403.
1985: Bernaerts R; De Clercq E; Balzarini J; Herdewijn P; Verbruggen A
Incorporation of carbocyclic (E)-5-(2-iodovinyl)-2'-deoxyuridine (C-IVDU) into DNA of herpes simplex virus-infected cells.
Antiviral research 1985;Suppl 1():51-6.

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