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Erik De Clercq
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331
Balzarini, Jan
141
Pannecouque, Christophe
108
Neyts, Johan
95
Andrei, Graciela
94
Snoeck, Robert
64
Naesens, Lieve
53
Schols, Dominique
50
McGuigan, Christopher
45
Witvrouw, Myriam
39
Vandamme, Anne-Mieke
33
Hatse, Sigrid
33
Camarasa, María-José
29
debyser, zeger
25
Dimmock, Jonathan
23
Velázquez, Sonsoles
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All Publications
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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.
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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.
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2009: Zhan Peng; Liu Xinyong; Fang Zengjun; Li Zhenyu; Pannecouque Christophe; De Clercq Erik
Synthesis and anti-HIV activity evaluation of 2-(4-(naphthalen-2-yl)-1,2,3-thiadiazol-5-ylthio)-N-acetamides as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
European journal of medicinal chemistry 2009;44(11):4648-53.
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2009: Cullen Matthew D; Ho William C; Bauman Joseph D; Das Kalyan; Arnold Eddy; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase.
Journal of medicinal chemistry 2009;52(20):6467-73.
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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.
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2009: De Clercq Erik
The history of antiretrovirals: key discoveries over the past 25 years.
Reviews in medical virology 2009;19(5):287-99.
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2009: Zhan Peng; Liu Xinyong; Fang Zengjun; Pannecouque Christophe; De Clercq Erik
1,2,3-Selenadiazole thioacetanilides: synthesis and anti-HIV activity evaluation.
Bioorganic & medicinal chemistry 2009;17(17):6374-9.
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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.
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2009: Karakus Sevgi; Güniz Küçükgüzel S; Küçükgüzel Ilkay; De Clercq Erik; Pannecouque Christophe; Andrei Graciela; Snoeck Robert; Sahin Fikrettin; Bayrak Omer Faruk
Synthesis, antiviral and anticancer activity of some novel thioureas derived from N-(4-nitro-2-phenoxyphenyl)-methanesulfonamide.
European journal of medicinal chemistry 2009;44(9):3591-5.
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2009: Shahar Yar M; Mustaqeem Abdullah M; Husain A; Bhakht M Afroz; De Clercq Erik
Synthesis and evaluation of in vitro antiviral activity of 2-[3-(substituted phenyl)-4,5-dihydro-1H-5-pyrazolyl]benzofuran-3-yl chloride derivatives.
Journal of enzyme inhibition and medicinal chemistry 2009;24(4):949-56.
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2009: Ostrowski Tomasz; Golankiewicz Bozenna; De Clercq Erik; Andrei Graciela; Snoeck Robert
Synthesis and anti-VZV activity of 6-heteroaryl derivatives of tricyclic acyclovir and 9-{[cis-1',2'-bis(hydroxymethyl)cycloprop-1'-yl]methyl}guanine analogues.
European journal of medicinal chemistry 2009;44(8):3313-7.
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2009: Zhan Peng; Li Zhenyu; Liu Xinyong; De Clercq Erik
Sulfanyltriazole/tetrazoles: a promising class of HIV-1 NNRTIs.
Mini reviews in medicinal chemistry 2009;9(8):1014-23.
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2009: De Clercq Erik
Another ten stories in antiviral drug discovery (part C): "Old" and "new" antivirals, strategies, and perspectives.
Medicinal research reviews 2009;29(4):611-45.
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2009: De Clercq Erik
Antiviral drug discovery: ten more compounds, and ten more stories (part B).
Medicinal research reviews 2009;29(4):571-610.
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2009: Paeshuyse Jan; Letellier Carine; Froeyen Matheus; Dutartre Hélène; Vrancken Robert; Canard Bruno; De Clercq Erik; Gueiffier Alain; Teulade Jean-Claude; Herdewijn Piet; Puerstinger Gerhard; Koenen Frank; Kerkhofs Pierre; Baraldi Pier Giovanni; Neyts Johan
A pyrazolotriazolopyrimidinamine inhibitor of bovine viral diarrhea virus replication that targets the viral RNA-dependent RNA polymerase.
Antiviral research 2009;82(3):141-7.
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2009: De Clercq Erik
The AMD3100 story: the path to the discovery of a stem cell mobilizer (Mozobil).
Biochemical pharmacology 2009;77(11):1655-64.
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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.
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2009: Santos Cledir R; Capela Rita; Pereira Cláudia S G P; Valente Emília; Gouveia Luís; Pannecouque Christophe; De Clercq Erik; Moreira Rui; Gomes Paula
Structure-activity relationships for dipeptide prodrugs of acyclovir: implications for prodrug design.
European journal of medicinal chemistry 2009;44(6):2339-46.
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2009: Mahajan Dharmesh H; Pannecouque Christophe; De Clercq Erik; Chikhalia Kishor H
Synthesis and studies of new 2-(coumarin-4-yloxy)-4,6-(substituted)-S-triazine derivatives as potential anti-HIV agents.
Archiv der Pharmazie 2009;342(5):281-90.
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2009: Vliegen Inge; Paeshuyse Jan; De Burghgraeve Tine; Lehman Laura S; Paulson Matthew; Shih I-Hung; Mabery Eric; Boddeker Nina; De Clercq Erik; Reiser Hans; Oare David; Lee William A; Zhong Weidong; Bondy Steven; Pürstinger Gerhard; Neyts Johan
Substituted imidazopyridines as potent inhibitors of HCV replication.
Journal of hepatology 2009;50(5):999-1009.
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2009: De Palma Armando M; Thibaut Hendrik Jan; van der Linden Lonneke; Lanke Kjerstin; Heggermont Ward; Ireland Stephen; Andrews Robert; Arimilli Murty; Al-Tel Taleb H; De Clercq Erik; van Kuppeveld Frank; Neyts Johan
Mutations in the nonstructural protein 3A confer resistance to the novel enterovirus replication inhibitor TTP-8307.
Antimicrobial agents and chemotherapy 2009;53(5):1850-7.
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2009: Zhang Jiyan; Liu Xinyong; De Clercq Erik
Capsid (CA) protein as a novel drug target: recent progress in the research of HIV-1 CA inhibitors.
Mini reviews in medicinal chemistry 2009;9(4):510-8.
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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.
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2009: Andrei Graciella; De Clercq Erik; Snoeck Robert
Drug targets in cytomegalovirus infection.
Infectious disorders drug targets 2009;9(2):201-22.
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2009: Duque María D; Camps Pelayo; Profire Lenuta; Montaner Silvia; Vázquez Santiago; Sureda Francesc X; Mallol Jordi; López-Querol Marta; Naesens Lieve; De Clercq Erik; Prathalingam S Radhika; Kelly John M
Synthesis and pharmacological evaluation of (2-oxaadamant-1-yl)amines.
Bioorganic & medicinal chemistry 2009;17(8):3198-206.
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2009: De Clercq Erik
Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV.
International journal of antimicrobial agents 2009;33(4):307-20.
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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.
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2009: Wang Yan; Liu Xin-Yong; De Clercq Erik
Role of the HIV-1 positive elongation factor P-TEFb and inhibitors thereof.
Mini reviews in medicinal chemistry 2009;9(3):379-85.
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2009: Khan Abid; Nicholson Gary; Greenman John; Madden Leigh; McRobbie Graeme; Pannecouque Christophe; De Clercq Erik; Ullom Robert; Maples Danny L; Maples Randall D; Silversides Jon D; Hubin Timothy J; Archibald Stephen J
Binding optimization through coordination chemistry: CXCR4 chemokine receptor antagonists from ultrarigid metal complexes.
Journal of the American Chemical Society 2009;131(10):3416-7.
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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.
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2009: Deng Bo-Liang; Zhao Yujie; Hartman Tracy L; Watson Karen; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
Synthesis of alkenyldiarylmethanes (ADAMs) containing benzo[d]isoxazole and oxazolidin-2-one rings, a new series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
European journal of medicinal chemistry 2009;44(3):1210-4.
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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.
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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.
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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.
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2009: Mingyan Yu; Xinyong Liu; De Clercq Erik
NF-kappaB: the inducible factors of HIV-1 transcription and their inhibitors.
Mini reviews in medicinal chemistry 2009;9(1):60-9.
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2009: Cao Yuan; Liu Xinyong; De Clercq Erik
Cessation of HIV-1 transcription by inhibiting regulatory protein Rev-mediated RNA transport.
Current HIV research 2009;7(1):101-8.
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2009: Bannwarth Ludovic; Rose Thierry; Dufau Laure; Vanderesse Régis; Dumond Julien; Jamart-Grégoire Brigitte; Pannecouque Christophe; De Clercq Erik; Reboud-Ravaux Michèle
Dimer disruption and monomer sequestration by alkyl tripeptides are successful strategies for inhibiting wild-type and multidrug-resistant mutated HIV-1 proteases.
Biochemistry 2009;48(2):379-87.
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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.
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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.
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2009: Zhan Peng; Liu Xinyong; Li Zhenyu; Pannecouque Christophe; De Clercq Erik
Design strategies of novel NNRTIs to overcome drug resistance.
Current medicinal chemistry 2009;16(29):3903-17.
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2009: De Clercq E
Interferon: the quintessence of a quinquagenarian.
Verhandelingen - Koninklijke Academie voor Geneeskunde van België 2009;71(1-2):5-14.
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2009: De Clercq Erik
Looking back in 2009 at the dawning of antiviral therapy now 50 years ago an historical perspective.
Advances in virus research 2009;73():1-53.
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2009: De Clercq E; Neyts J
Antiviral agents acting as DNA or RNA chain terminators.
Handbook of experimental pharmacology 2009;(189):53-84.
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2008: Kolocouris Antonios; Spearpoint Philip; Martin Stephen R; Hay Alan J; López-Querol Marta; Sureda Francesc X; Padalko Elizaveta; Neyts Johan; De Clercq Erik
Comparisons of the influenza virus A M2 channel binding affinities, anti-influenza virus potencies and NMDA antagonistic activities of 2-alkyl-2-aminoadamantanes and analogues.
Bioorganic & medicinal chemistry letters 2008;18(23):6156-60.
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2008: Gammon Don B; Snoeck Robert; Fiten Pierre; Krecmerová Marcela; Holý Antonín; De Clercq Erik; Opdenakker Ghislain; Evans David H; Andrei Graciela
Mechanism of antiviral drug resistance of vaccinia virus: identification of residues in the viral DNA polymerase conferring differential resistance to antipoxvirus drugs.
Journal of virology 2008;82(24):12520-34.
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2008: Rawal Ravindra K; Tripathi Rajkamal; Katti S B; Pannecouque Christophe; De Clercq Erik
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
European journal of medicinal chemistry 2008;43(12):2800-6.
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2008: Véron Jean-Baptiste; Allouchi Hassan; Enguehard-Gueiffier Cécile; Snoeck Robert; Andrei Graciela; De Clercq Erik; Gueiffier Alain
Influence of 6- or 8-substitution on the antiviral activity of 3-arylalkylthiomethylimidazo[1,2-a]pyridine against human cytomegalovirus (CMV) and varicella-zoster virus (VZV): part II.
Bioorganic & medicinal chemistry 2008;16(21):9536-45.
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2008: Lenaerts Liesbeth; De Clercq Erik; Naesens Lieve
Clinical features and treatment of adenovirus infections.
Reviews in medical virology 2008;18(6):357-74.
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2008: De Clercq Erik
The discovery of antiviral agents: ten different compounds, ten different stories.
Medicinal research reviews 2008;28(6):929-53.
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2008: De Palma Armando M; Vliegen Inge; De Clercq Erik; Neyts Johan
Selective inhibitors of picornavirus replication.
Medicinal research reviews 2008;28(6):823-84.
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2008: Yu Fang; Liu Xinyong; Zhan Peng; De Clercq Erik
Recent advances in the research of HIV-1 RNase H inhibitors.
Mini reviews in medicinal chemistry 2008;8(12):1243-51.
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2008: Zhan Peng; Liu Xinyong; Cao Yuan; Wang Yan; Pannecouque Christophe; De Clercq Erik
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(20):5368-71.
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2008: Naesens Lieve; Andrei Graciela; Votruba Ivan; Krecmerová Marcela; Holý Antonín; Neyts Johan; De Clercq Erik; Snoeck Robert
Intracellular metabolism of the new antiviral compound 1-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]-5-azacytosine.
Biochemical pharmacology 2008;76(8):997-1005.
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2008: Gawin Rafal; De Clercq Erik; Naesens Lieve; Koszytkowska-Stawinska Mariola
Synthesis and antiviral evaluation of acyclic azanucleosides developed from sulfanilamide as a lead structure.
Bioorganic & medicinal chemistry 2008;16(18):8379-89.
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2008: De Clercq Erik
Emerging antiviral drugs.
Expert opinion on emerging drugs 2008;13(3):393-416.
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2008: Zoidis Grigoris; Tsotinis Andrew; Kolocouris Nicolas; Kelly John M; Prathalingam S Radhika; Naesens Lieve; De Clercq Erik
Design and synthesis of bioactive 1,2-annulated adamantane derivatives.
Organic & biomolecular chemistry 2008;6(17):3177-85.
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2008: Rawal Ravindra K; Tripathi Rajkamal; Kulkarni Smitha; Paranjape R; Katti S B; Pannecouque Christophe; De Clercq Erik
2-(2,6-Dihalo-phenyl)-3-heteroaryl-2-ylmethyl-1, 3-thiazolidin-4-ones: anti-HIV agents.
Chemical biology & drug design 2008;72(2):147-54.
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2008: Monforte Anna-Maria; Rao Angela; Logoteta Patrizia; Ferro Stefania; De Luca Laura; Barreca Maria Letizia; Iraci Nunzio; Maga Giovanni; De Clercq Erik; Pannecouque Christophe; Chimirri Alba
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
Bioorganic & medicinal chemistry 2008;16(15):7429-35.
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2008: Dal Pozzo Fabiana; Andrei Graciela; Daelemans Dirk; Winkler Michael; Piette Jacques; De Clercq Erik; Snoeck Robert
Fluorescence-based antiviral assay for the evaluation of compounds against vaccinia virus, varicella zoster virus and human cytomegalovirus.
Journal of virological methods 2008;151(1):66-73.
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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.
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2008: Santos Cledir; Morais José; Gouveia Luís; de Clercq Erik; Pannecouque Christophe; Nielsen Carsten Uhd; Steffansen Bente; Moreira Rui; Gomes Paula
Dipeptide derivatives of AZT: synthesis, chemical stability, activation in human plasma, hPEPT1 affinity, and antiviral activity.
ChemMedChem 2008;3(6):970-8.
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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.
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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.
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2008: De Palma Armando M; Heggermont Ward; Lanke Kjerstin; Coutard Bruno; Bergmann Mirko; Monforte Anna-Maria; Canard Bruno; De Clercq Erik; Chimirri Alba; Pürstinger Gerhard; Rohayem Jacques; van Kuppeveld Frank; Neyts Johan
The thiazolobenzimidazole TBZE-029 inhibits enterovirus replication by targeting a short region immediately downstream from motif C in the nonstructural protein 2C.
Journal of virology 2008;82(10):4720-30.
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2008: De Palma Armando M; Pürstinger Gerhard; Wimmer Eva; Patick Amy K; Andries Koen; Rombaut Bart; De Clercq Erik; Neyts Johan
Potential use of antiviral agents in polio eradication.
Emerging infectious diseases 2008;14(4):545-51.
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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.
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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.
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2008: Leyssen Pieter; De Clercq Erik; Neyts Johan
Molecular strategies to inhibit the replication of RNA viruses.
Antiviral research 2008;78(1):9-25.
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2008: Lenaerts L; Kelchtermans H; Geboes L; Matthys P; Verbeken E; De Clercq E; Naesens L
Recovery of humoral immunity is critical for successful antiviral therapy in disseminated mouse adenovirus type 1 infection.
Antimicrobial agents and chemotherapy 2008;52(4):1462-71.
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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.
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2008: Liu Xin-yong; Yan Ren-zhang; Wang Yan; Zhan Peng; De Clercq Erik; Pannecouque Christophe; Witvrouw Myriam; Molina Maria Teresa; Vega Salvador
Synthesis and anti-HIV activity evaluation of novel 2,4-disubstituted 7-methyl-1,1,3-trioxo-2,4-dihydro-pyrazolo-[4,5-e][1,2]thiadiazines.
Archiv der Pharmazie 2008;341(4):216-22.
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2008: Ptak Roger G; Gallay Philippe A; Jochmans Dirk; Halestrap Andrew P; Ruegg Urs T; Pallansch Luke A; Bobardt Michael D; de Béthune Marie-Pierre; Neyts Johan; De Clercq Erik; Dumont Jean-Maurice; Scalfaro Pietro; Besseghir Kamel; Wenger Roland M; Rosenwirth Brigitte
Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent.
Antimicrobial agents and chemotherapy 2008;52(4):1302-17.
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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.
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2008: Cullen Matthew D; Cheung York-Fong; Houslay Miles D; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
Bioorganic & medicinal chemistry letters 2008;18(4):1530-3.
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2008: Hwu Jih Ru; Singha Raghunath; Hong Shih Ching; Chang Yung Hsiung; Das Asish R; Vliegen Inge; De Clercq Erik; Neyts Johan
Synthesis of new benzimidazole-coumarin conjugates as anti-hepatitis C virus agents.
Antiviral research 2008;77(2):157-62.
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2008: Küçükgüzel Ilkay; Tatar Esra; Küçükgüzel S Güniz; Rollas Sevim; De Clercq Erik
Synthesis of some novel thiourea derivatives obtained from 5-[(4-aminophenoxy)methyl]-4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones and evaluation as antiviral/anti-HIV and anti-tuberculosis agents.
European journal of medicinal chemistry 2008;43(2):381-92.
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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.
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2008: Cullen Matthew D; Sarkar Taradas; Hamel Ernest; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
Bioorganic & medicinal chemistry letters 2008;18(2):469-73.
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2008: Férir Geoffrey; Kaptein Suzanne; Neyts Johan; De Clercq Erik
Antiviral treatment of chronic hepatitis B virus infections: the past, the present and the future.
Reviews in medical virology 2008;18(1):19-34.
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2008: Lin Yongqiang; Liu Xinyong; Yan Renzhang; Li Jin; Pannecouque Christophe; Witvrouw Myriam; De Clercq Erik
Synthesis and anti-HIV evaluation of novel 1,3-disubstituted thieno[3,2-c][1,2,6]thiadiazin-4(3H)-one 2,2-dioxides(TTDDs).
Bioorganic & medicinal chemistry 2008;16(1):157-63.
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2008: Aubin Yoann; Audran Gérard; Monti Honoré; De Clercq Erik
Chemoenzymatic synthesis and antiviral evaluation of conformationally constrained and 3'-methyl-branched carbanucleosides using both enantiomers of the same building block.
Bioorganic & medicinal chemistry 2008;16(1):374-81.
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2008: Lagoja Irene M; De Clercq Erik
Anti-influenza virus agents: synthesis and mode of action.
Medicinal research reviews 2008;28(1):1-38.
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2008: Fogt Joanna; Januszczyk Piotr; Framski Grzegorz; Onishi Tomoyuki; Izawa Kunisuke; De Clercq Erik; Neyts Johan; Boryski Jerzy
Synthesis and antiviral activity of novel derivatives of 2'-beta-C-methylcytidine.
Nucleic acids symposium series (2004) 2008;(52):605-6.
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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.
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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: De Clercq Erik; Field Hugh J
Antiviral Chemistry & Chemotherapy's current antiviral agents FactFile (2nd edition): retroviruses and hepadnaviruses.
Antiviral chemistry & chemotherapy 2008;19(2):75-105.
-
2008: De Clercq Erik; Field Hugh J
Antiviral Chemistry & Chemotherapy's current antiviral agents FactFile 2008 (2nd edition): RNA viruses.
Antiviral chemistry & chemotherapy 2008;19(2):63-74.
-
2008: Zhan Peng; Liu Xinyong; De Clercq Erik
Recent advances in antiviral activity of benzo/heterothiadiazine dioxide derivatives.
Current medicinal chemistry 2008;15(15):1529-40.
-
2008: Pannecouque Christophe; Daelemans Dirk; De Clercq Erik
Tetrazolium-based colorimetric assay for the detection of HIV replication inhibitors: revisited 20 years later.
Nature protocols 2008;3(3):427-34.
-
2007: Al-Soud Yaseen A; Al-Masoudi Najim A; Hassan Hamed Gh; De Clercq Erik; Pannecouque Christophe
Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives.
Acta pharmaceutica (Zagreb, Croatia) 2007;57(4):379-93.
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2007: De Clercq Erik
The design of drugs for HIV and HCV.
Nature reviews. Drug discovery 2007;6(12):1001-18.
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2007: Pérez-Castro Isabel; Caamaño Olga; Fernández Franco; García Marcos D; López Carmen; De Clercq Erik
Synthesis of 4-substituted-1,2,3-triazole carbanucleoside analogues of ribavirin via click chemistry.
Organic & biomolecular chemistry 2007;5(23):3805-13.
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2007: Duraffour Sophie; Snoeck Robert; Krecmerová Marcela; van Den Oord Joost; De Vos Rita; Holy Antonín; Crance Jean-Marc; Garin Daniel; De Clercq Erik; Andrei Graciela
Activities of several classes of acyclic nucleoside phosphonates against camelpox virus replication in different cell culture models.
Antimicrobial agents and chemotherapy 2007;51(12):4410-9.
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2007: McRobbie Graeme; Valks Gina C; Empson Christopher J; Khan Abid; Silversides Jon D; Pannecouque Christophe; De Clercq Erik; Fiddy Steven G; Bridgeman Adam J; Young Nigel A; Archibald Stephen J
Probing key coordination interactions: configurationally restricted metal activated CXCR4 antagonists.
Dalton transactions (Cambridge, England : 2003) 2007;(43):5008-18.
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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.
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2007: Véron Jean-Baptiste; Enguehard-Gueiffier Cécile; Snoeck Robert; Andrei Graciela; De Clercq Erik; Gueiffier Alain
Influence of 6 or 8-substitution on the antiviral activity of 3-phenethylthiomethylimidazo[1,2-a]pyridine against human cytomegalovirus (HCMV) and varicella-zoster virus (VZV).
Bioorganic & medicinal chemistry 2007;15(22):7209-19.
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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.
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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.
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2007: Paeshuyse Jan; Chezal Jean-Michel; Froeyen Matheus; Leyssen Pieter; Dutartre Hélène; Vrancken Robert; Canard Bruno; Letellier Carine; Li Tong; Mittendorfer Harald; Koenen Frank; Kerkhofs Pierre; De Clercq Erik; Herdewijn Piet; Puerstinger Gerhard; Gueiffier Alain; Chavignon Olivier; Teulade Jean-Claude; Neyts Johan
The imidazopyrrolopyridine analogue AG110 is a novel, highly selective inhibitor of pestiviruses that targets the viral RNA-dependent RNA polymerase at a hot spot for inhibition of viral replication.
Journal of virology 2007;81(20):11046-53.
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2007: Painter George R; Almond Merrick R; Trost Lawrence C; Lampert Bernhard M; Neyts Johan; De Clercq Erik; Korba Brent E; Aldern Kathy A; Beadle James R; Hostetler Karl Y
Evaluation of hexadecyloxypropyl-9-R-[2-(Phosphonomethoxy)propyl]- adenine, CMX157, as a potential treatment for human immunodeficiency virus type 1 and hepatitis B virus infections.
Antimicrobial agents and chemotherapy 2007;51(10):3505-9.
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2007: Puerstinger Gerhard; Paeshuyse Jan; Heinrich Susanne; Mohr Joachim; Schraffl Nicole; De Clercq Erik; Neyts Johan
Antiviral 2,5-disubstituted imidazo[4,5-c]pyridines: further optimization of anti-hepatitis C virus activity.
Bioorganic & medicinal chemistry letters 2007;17(18):5111-4.
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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.
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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.
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2007: Kolocouris Nicolas; Zoidis Grigoris; Foscolos George B; Fytas George; Prathalingham S Radhika; Kelly John M; Naesens Lieve; De Clercq Erik
Design and synthesis of bioactive adamantane spiro heterocycles.
Bioorganic & medicinal chemistry letters 2007;17(15):4358-62.
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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.
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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.
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2007: Rawal Ravindra K; Tripathi Raj Kamal; Katti S B; Pannecouque Christophe; De Clercq Erik
Synthesis and biological evaluation of 2,3-diaryl substituted-1,3-thiazolidin-4-ones as anti-HIV agents.
Medicinal chemistry (Shariqah (United Arab Emirates)) 2007;3(4):355-63.
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2007: Kang Soon Bang; De Clercq Erik; Lakshman Mahesh K
Pd-catalyzed C-C bond-forming reactions of thymidine mesitylene sulfonate.
The Journal of organic chemistry 2007;72(15):5724-30.
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2007: Sakamoto Takeshi; Cullen Matthew D; Hartman Tracy L; Watson Karen M; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
Synthesis and anti-HIV activity of new metabolically stable alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors incorporating N-methoxy imidoyl halide and 1,2,4-oxadiazole systems.
Journal of medicinal chemistry 2007;50(14):3314-21.
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2007: Shi Minyi; Wang Xin; De Clercq Erik; Takao Sonshin; Baba Masanori
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
Antimicrobial agents and chemotherapy 2007;51(7):2600-4.
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2007: Bugatti Antonella; Urbinati Chiara; Ravelli Cosetta; De Clercq Erik; Liekens Sandra; Rusnati Marco
Heparin-mimicking sulfonic acid polymers as multitarget inhibitors of human immunodeficiency virus type 1 Tat and gp120 proteins.
Antimicrobial agents and chemotherapy 2007;51(7):2337-45.
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2007: Küçükgüzel S Güniz; Küçükgüzel Ilkay; Tatar Esra; Rollas Sevim; Sahin Fikrettin; Güllüce Medine; De Clercq Erik; Kabasakal Levent
Synthesis of some novel heterocyclic compounds derived from diflunisal hydrazide as potential anti-infective and anti-inflammatory agents.
European journal of medicinal chemistry 2007;42(7):893-901.
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2007: Dal Pozzo Fabiana; Andrei Graciela; Lebeau Ilya; Beadle James R; Hostetler Karl Y; De Clercq Erik; Snoeck Robert
In vitro evaluation of the anti-orf virus activity of alkoxyalkyl esters of CDV, cCDV and (S)-HPMPA.
Antiviral research 2007;75(1):52-7.
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2007: De Clercq Erik
The acyclic nucleoside phosphonates from inception to clinical use: historical perspective.
Antiviral research 2007;75(1):1-13.
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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.
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2007: De Clercq Erik; Neyts Johan
Avian influenza A (H5N1) infection: targets and strategies for chemotherapeutic intervention.
Trends in pharmacological sciences 2007;28(6):280-5.
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2007: Andrei G; Fiten P; Goubau P; van Landuyt H; Gordts B; Selleslag D; De Clercq E; Opdenakker G; Snoeck R
Dual infection with polyomavirus BK and acyclovir-resistant herpes simplex virus successfully treated with cidofovir in a bone marrow transplant recipient.
Transplant infectious disease : an official journal of the Transplantation Society 2007;9(2):126-31.
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2007: Lebeau Ilya; Andrei Graciela; Krecmerová Marcela; De Clercq Erik; Holy Antonin; Snoeck Robert
Inhibitory activities of three classes of acyclic nucleoside phosphonates against murine polyomavirus and primate simian virus 40 strains.
Antimicrobial agents and chemotherapy 2007;51(6):2268-73.
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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.
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2007: Rawal Ravindra K; Tripathi Rajkamal; Katti S B; Pannecouque Christophe; De Clercq Erik
Synthesis and evaluation of 2-(2,6-dihalophenyl)-3-pyrimidinyl-1,3-thiazolidin-4-one analogues as anti-HIV-1 agents.
Bioorganic & medicinal chemistry 2007;15(9):3134-42.
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2007: González-Díaz Humberto; Bonet Isis; Terán Carmen; De Clercq Erik; Bello Rafael; García Maria M; Santana Lourdes; Uriarte Eugenio
ANN-QSAR model for selection of anticancer leads from structurally heterogeneous series of compounds.
European journal of medicinal chemistry 2007;42(5):580-5.
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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.
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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.
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2007: Daelemans Dirk; Lu Richard; De Clercq Erik; Engelman Alan
Characterization of a replication-competent, integrase-defective human immunodeficiency virus (HIV)/simian virus 40 chimera as a powerful tool for the discovery and validation of HIV integrase inhibitors.
Journal of virology 2007;81(8):4381-5.
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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.
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2007: Hatse Sigrid; Huskens Dana; Princen Katrien; Vermeire Kurt; Bridger Gary J; De Clercq Erik; Rosenkilde Mette M; Schwartz Thue W; Schols Dominique
Modest human immunodeficiency virus coreceptor function of CXCR3 is strongly enhanced by mimicking the CXCR4 ligand binding pocket in the CXCR3 receptor.
Journal of virology 2007;81(7):3632-9.
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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.
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2007: De Clercq E
Acyclic nucleoside phosphonates: past, present and future. Bridging chemistry to HIV, HBV, HCV, HPV, adeno-, herpes-, and poxvirus infections: the phosphonate bridge.
Biochemical pharmacology 2007;73(7):911-22.
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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.
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2007: Liekens Sandra; Gijsbers Sofie; Vanstreels Els; Daelemans Dirk; De Clercq Erik; Hatse Sigrid
The nucleotide analog cidofovir suppresses basic fibroblast growth factor (FGF2) expression and signaling and induces apoptosis in FGF2-overexpressing endothelial cells.
Molecular pharmacology 2007;71(3):695-703.
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2007: Ying Chunxiao; Colonno Richard; De Clercq Erik; Neyts Johan
Ribavirin and mycophenolic acid markedly potentiate the anti-hepatitis B virus activity of entecavir.
Antiviral research 2007;73(3):192-6.
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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.
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2007: Harinantenaina Liva; Asakawa Yoshinori; De Clercq Erik
Cinnamacrins A-C, cinnafragrin D, and cytostatic metabolites with alpha-glucosidase inhibitory activity from Cinnamosma macrocarpa.
Journal of natural products 2007;70(2):277-82.
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2007: De Palma Armando M; Heggermont Ward; Leyssen Pieter; Pürstinger Gerhard; Wimmer Eva; De Clercq Erik; Rao Angela; Monforte Anna-Maria; Chimirri Alba; Neyts Johan
Anti-enterovirus activity and structure-activity relationship of a series of 2,6-dihalophenyl-substituted 1H,3H-thiazolo[3,4-a]benzimidazoles.
Biochemical and biophysical research communications 2007;353(3):628-32.
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2007: Rawal Ravindra K; Tripathi Rajkamal; Katti S B; Pannecouque Christophe; De Clercq Erik
Design, synthesis, and evaluation of 2-aryl-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
Bioorganic & medicinal chemistry 2007;15(4):1725-31.
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2007: Tataridis Dimitrios; Fytas George; Kolocouris Antonios; Fytas Christos; Kolocouris Nicolas; Foscolos George B; Padalko Elizaveta; Neyts Johan; De Clercq Erik
Influence of an additional 2-amino substituent of the 1-aminoethyl pharmacophore group on the potency of rimantadine against influenza virus A.
Bioorganic & medicinal chemistry letters 2007;17(3):692-6.
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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.
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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.
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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.
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2007: Puerstinger Gerhard; Paeshuyse Jan; De Clercq Erik; Neyts Johan
Antiviral 2,5-disubstituted imidazo[4,5-c]pyridines: from anti-pestivirus to anti-hepatitis C virus activity.
Bioorganic & medicinal chemistry letters 2007;17(2):390-3.
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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.
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2007: Duraffour Sophie; Snoeck Robert; de Vos Rita; van Den Oord Joost J; Crance Jean-Marc; Garin Daniel; Hruby Dennis E; Jordan Robert; De Clercq Erik; Andrei Graciela
Activity of the anti-orthopoxvirus compound ST-246 against vaccinia, cowpox and camelpox viruses in cell monolayers and organotypic raft cultures.
Antiviral therapy 2007;12(8):1205-16.
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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.
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2007: Jahnz-Wechmann Zofia; Boryski Jerzy; Izawa Kunisuke; Onishi Tomoyuki; Neyts Johan; De Clercq Erik
New analogs of acyclovir substituted at the side chain.
Nucleosides, nucleotides & nucleic acids 2007;26(8-9):917-20.
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2007: Garozzo Adriana; Cutri Christian C C; Pannecouque Christophe; Castro Angelo; Guerrera Francesco; De Clercq Erik
Isothiazole derivatives as antiviral agents.
Antiviral chemistry & chemotherapy 2007;18(5):277-83.
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2007: Wu Jingde; Liu Xinyong; Cheng Xianchao; Cao Yuan; Wang Defeng; Li Zhong; Xu Wenfang; Pannecouque Christophe; Witvrouw Myriam; De Clercq Erik
Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential HIV-1 NNRTIs.
Molecules (Basel, Switzerland) 2007;12(8):2003-16.
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2007: Jarrahpour Aliasghar; Khalili Dariush; De Clercq Erik; Salmi Chanaz; Brunel Jean Michel
Synthesis, antibacterial, antifungal and antiviral activity evaluation of some new bis-Schiff bases of isatin and their derivatives.
Molecules (Basel, Switzerland) 2007;12(8):1720-30.
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2007: Al-Masoudi Najim A; Al-Soud Yaseen A; De Clercq Erik; Pannecouque Christophe
Nitroimidazoles Part 6. Synthesis, structure and in vitro anti-HIV activity of new 5-substituted piperazinyl-4-nitroimidazole derivatives.
Antiviral chemistry & chemotherapy 2007;18(4):191-200.
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2007: Andrei Gracíela; Fiten Pierre; Froeyen Matheus; De Clercq Erik; Opdenakker Ghislain; Snoeck Robert
DNA polymerase mutations in drug-resistant herpes simplex virus mutants determine in vivo neurovirulence and drug-enzyme interactions.
Antiviral therapy 2007;12(5):719-32.
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2007: De Clercq E
Anti-HIV drugs.
Verhandelingen - Koninklijke Academie voor Geneeskunde van België 2007;69(2):81-104.
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2007: De Clercq E
AIDS in the Third World: how to stop the HIV infection?
Verhandelingen - Koninklijke Academie voor Geneeskunde van België 2007;69(2):65-80.
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2007: Moukha-Chafiq Omar; Taha Mohamed Labd; Mouna Abdelmalek; Lazrek Hassan Bihi; Vasseur Jean-Jacques; De Clercq Erik
Synthesis and biological evaluation of some alpha-[6-(1'-carbamoylalkylthio)-1 H-pyrazolo[3,4-D]pyrimidin-4-yl]thioalkylcarboxamide acyclonucleosides.
Nucleosides, nucleotides & nucleic acids 2007;26(4):335-45.
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2007: Al-Masoudi Najim A; Al-Soud Yaseen A; Ali Ibrahim A I; Schuppler Thilo; Pannecouque Christoph; De Clercq Erik
New AZT analogues having 5'-alkylsulfonyl groups: synthesis and anti-HIV activity.
Nucleosides, nucleotides & nucleic acids 2007;26(3):223-30.
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2007: Koszytkowska-Stawinska Mariola; Kaleta Katarzyna; Sas Wojciech; De Clercq Erik
Synthesis and antiviral properties of aza-analogues of acyclovir.
Nucleosides, nucleotides & nucleic acids 2007;26(1):51-64.
-
2006: De Clercq Erik; Naesens Lieve
In search of effective anti-HHV-6 agents.
Journal of clinical virology : the official publication of the Pan American Society for Clinical Virology 2006;37 Suppl 1():S82-6.
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2006: Naesens Lieve; Bonnafous Pascale; Agut Henri; De Clercq Erik
Antiviral activity of diverse classes of broad-acting agents and natural compounds in HHV-6-infected lymphoblasts.
Journal of clinical virology : the official publication of the Pan American Society for Clinical Virology 2006;37 Suppl 1():S69-75.
-
2006: De Clercq Erik
Antiviral agents active against influenza A viruses.
Nature reviews. Drug discovery 2006;5(12):1015-25.
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2006: Horejsí Katerina; Andrei Graciela; De Clercq Erik; Snoeck Robert; Pohl Radek; Holý Antonín
Tricyclic etheno analogs of PMEG and PMEDAP: synthesis and biological activity.
Bioorganic & medicinal chemistry 2006;14(23):8057-65.
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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.
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2006: Yan Ren-Zhang; Liu Xin-Yong; Xu Wen-Fang; Pannecouque Christophe; Witvrouw Myriam; De Clercq Erik
Synthesis and anti-HIV evaluation of the novel 2-(m-chlorobenzyl)-4-substituted-7-methyl-1, 1, 3-trioxo-pyrazolo[4, 5-e] [1, 2, 4]thiadiazines.
Archives of pharmacal research 2006;29(11):957-62.
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2006: Valks Gina C; McRobbie Graeme; Lewis Elizabeth A; Hubin Timothy J; Hunter Tina M; Sadler Peter J; Pannecouque Christophe; De Clercq Erik; Archibald Stephen J
Configurationally restricted bismacrocyclic CXCR4 receptor antagonists.
Journal of medicinal chemistry 2006;49(21):6162-5.
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2006: Canoa Pilar; González-Moa María J; Teijeira Marta; Terán Carmen; Uriarte Eugenio; Pannecouque Christophe; De Clercq Erik
Synthesis and anti-HIV activity of novel cyclopentenyl nucleoside analogues of 8-azapurine.
Chemical & pharmaceutical bulletin 2006;54(10):1418-20.
-
2006: Coelmont Lotte; Paeshuyse Jan; Windisch Marc P; De Clercq Erik; Bartenschlager Ralf; Neyts Johan
Ribavirin antagonizes the in vitro anti-hepatitis C virus activity of 2'-C-methylcytidine, the active component of valopicitabine.
Antimicrobial agents and chemotherapy 2006;50(10):3444-6.
-
2006: De Clercq Erik
The role of tenofovir in the prevention of HIV infections.
AIDS (London, England) 2006;20(15):1990-1.
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2006: Andrei Graciela; Gammon Don B; Fiten Pierre; De Clercq Erik; Opdenakker Ghislain; Snoeck Robert; Evans David H
Cidofovir resistance in vaccinia virus is linked to diminished virulence in mice.
Journal of virology 2006;80(19):9391-401.
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2006: Puerstinger Gerhard; Paeshuyse Jan; Herdewijn Piet; Rozenski Jef; De Clercq Erik; Neyts Johan
Substituted 5-benzyl-2-phenyl-5H-imidazo[4,5-c]pyridines: a new class of pestivirus inhibitors.
Bioorganic & medicinal chemistry letters 2006;16(20):5345-9.
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2006: Setaki Despina; Tataridis Dimitris; Stamatiou George; Kolocouris Antonios; Foscolos George B; Fytas George; Kolocouris Nicolas; Padalko Elizaveta; Neyts Johan; De Clercq Erik
Synthesis, conformational characteristics and anti-influenza virus A activity of some 2-adamantylsubstituted azacycles.
Bioorganic chemistry 2006;34(5):248-73.
-
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.
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2006: Naesens Lieve; Stephens Chad E; Andrei Graciela; Loregian Arianna; De Bolle Leen; Snoeck Robert; Sowell J Walter; De Clercq Erik
Antiviral properties of new arylsulfone derivatives with activity against human betaherpesviruses.
Antiviral research 2006;72(1):60-7.
-
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: De Clercq Erik
Interferon and its inducers--a never-ending story: "old" and "new" data in a new perspective.
The Journal of infectious diseases 2006;194 Suppl 1():S19-26.
-
2006: Paeshuyse Jan; Coelmont Lotte; Vliegen Inge; Van hemel Johan; Vandenkerckhove Jan; Peys Eric; Sas Benedikt; De Clercq Erik; Neyts Johan
Hemin potentiates the anti-hepatitis C virus activity of the antimalarial drug artemisinin.
Biochemical and biophysical research communications 2006;348(1):139-44.
-
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: Deng Bo-Liang; Hartman Tracy L; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Cushman Mark
Replacement of the metabolically labile methyl esters in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors with isoxazolone, isoxazole, oxazolone, or cyano substituents.
Journal of medicinal chemistry 2006;49(17):5316-23.
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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.
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2006: Lenaerts L; Daelemans D; Geukens N; De Clercq E; Naesens L
Mouse adenovirus type 1 attachment is not mediated by the coxsackie-adenovirus receptor.
FEBS letters 2006;580(16):3937-42.
-
2006: Lebeau Ilya; Andrei Graciela; Dal Pozzo Fabiana; Beadle James R; Hostetler Karl Y; De Clercq Erik; van den Oord Joost; Snoeck Robert
Activities of alkoxyalkyl esters of cidofovir (CDV), cyclic CDV, and (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine against orthopoxviruses in cell monolayers and in organotypic cultures.
Antimicrobial agents and chemotherapy 2006;50(7):2525-9.
-
2006: Al-Masoudi Najim A; Al-Soud Yaseen A; Kalogerakis Aris; Pannecouque Christophe; De Clercq Erik
Nitroimidazoles, part 2: Synthesis, antiviral and antitumor activity of new 4-nitroimidazoles.
Chemistry & biodiversity 2006;3(5):515-26.
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2006: Biot Christophe; Daher Wassim; Chavain Natascha; Fandeur Thierry; Khalife Jamal; Dive Daniel; De Clercq Erik
Design and synthesis of hydroxyferroquine derivatives with antimalarial and antiviral activities.
Journal of medicinal chemistry 2006;49(9):2845-9.
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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.
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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.
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2006: Zoidis Grigoris; Fytas Christos; Papanastasiou Ioannis; Foscolos George B; Fytas George; Padalko Elizaveta; De Clercq Erik; Naesens Lieve; Neyts Johan; Kolocouris Nicolas
Heterocyclic rimantadine analogues with antiviral activity.
Bioorganic & medicinal chemistry 2006;14(10):3341-8.
-
2006: Tabarrini Oriana; Manfroni Giuseppe; Fravolini Arnaldo; Cecchetti Violetta; Sabatini Stefano; De Clercq Erik; Rozenski Jef; Canard Bruno; Dutartre Hélène; Paeshuyse Jan; Neyts Johan
Synthesis and anti-BVDV activity of acridones as new potential antiviral agents.
Journal of medicinal chemistry 2006;49(8):2621-7.
-
2006: De Clercq Erik
Potential antivirals and antiviral strategies against SARS coronavirus infections.
Expert review of anti-infective therapy 2006;4(2):291-302.
-
2006: Paeshuyse Jan; Kaul Artur; De Clercq Erik; Rosenwirth Brigitte; Dumont Jean-Maurice; Scalfaro Pietro; Bartenschlager Ralf; Neyts Johan
The non-immunosuppressive cyclosporin DEBIO-025 is a potent inhibitor of hepatitis C virus replication in vitro.
Hepatology (Baltimore, Md.) 2006;43(4):761-70.
-
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: Leyssen Pieter; De Clercq Erik; Neyts Johan
The anti-yellow fever virus activity of ribavirin is independent of error-prone replication.
Molecular pharmacology 2006;69(4):1461-7.
-
2006: Deng Bo-Liang; Cullen Matthew D; Zhou Zhigang; Hartman Tracy L; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Fanwick Phillip E; Cushman Mark
Synthesis and anti-HIV activity of new alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors (NNRTIs) incorporating benzoxazolone and benzisoxazole rings.
Bioorganic & medicinal chemistry 2006;14(7):2366-74.
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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.
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2006: Küçükgüzel Güniz; Kocatepe Ayla; De Clercq Erik; Sahin Fikrettin; Güllüce Medine
Synthesis and biological activity of 4-thiazolidinones, thiosemicarbazides derived from diflunisal hydrazide.
European journal of medicinal chemistry 2006;41(3):353-9.
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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.
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2006: Guillerm Georges; Muzard Murielle; Glapski Cédric; Pilard Serge; De Clercq Erik
Inactivation of S-adenosyl-L-homocysteine hydrolase by 6'-cyano-5',6'-didehydro-6'-deoxyhomoadenosine and 6'-chloro-6'-cyano-5',6'-didehydro-6'-deoxyhomoadenosine. Antiviral and cytotoxic effects.
Journal of medicinal chemistry 2006;49(4):1223-6.
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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.
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2006: Stittelaar Koert J; Neyts Johan; Naesens Lieve; van Amerongen Geert; van Lavieren Rob F; Holý Antonin; De Clercq Erik; Niesters Hubert G M; Fries Edwin; Maas Chantal; Mulder Paul G H; van der Zeijst Ben A M; Osterhaus Albert D M E
Antiviral treatment is more effective than smallpox vaccination upon lethal monkeypox virus infection.
Nature 2006;439(7077):745-8.
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2006: González-Díaz Humberto; Viña Dolores; Santana Lourdes; de Clercq Erik; Uriarte Eugenio
Stochastic entropy QSAR for the in silico discovery of anticancer compounds: prediction, synthesis, and in vitro assay of new purine carbanucleosides.
Bioorganic & medicinal chemistry 2006;14(4):1095-107.
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2006: Rescifina Antonio; Chiacchio Maria A; Corsaro Antonino; De Clercq Erik; Iannazzo Daniela; Mastino Antonio; Piperno Anna; Romeo Giovanni; Romeo Roberto; Valveri Vincenza
Synthesis and biological activity of isoxazolidinyl polycyclic aromatic hydrocarbons: potential DNA intercalators.
Journal of medicinal chemistry 2006;49(2):709-15.
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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.
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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.
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2006: Paeshuyse Jan; Leyssen Pieter; Mabery Eric; Boddeker Nina; Vrancken Robert; Froeyen Matheus; Ansari Israrul H; Dutartre Hélène; Rozenski Jef; Gil Laura H V G; Letellier Carine; Lanford Robert; Canard Bruno; Koenen Frank; Kerkhofs Pierre; Donis Ruben O; Herdewijn Piet; Watson Julia; De Clercq Erik; Puerstinger Gerhard; Neyts Johan
A novel, highly selective inhibitor of pestivirus replication that targets the viral RNA-dependent RNA polymerase.
Journal of virology 2006;80(1):149-60.
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2006: De Clercq Erik; Field Hugh J
Antiviral prodrugs - the development of successful prodrug strategies for antiviral chemotherapy.
British journal of pharmacology 2006;147(1):1-11.
-
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.
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2006: Charlier Nathalie; De Clercq Erik; Neyts Johan
Mouse and hamster models for the study of therapy against flavivirus infections.
Novartis Foundation symposium 2006;277():218-29; discussion 229-32, 251-3.
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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: De Clercq Erik; Brancale Andrea; Hodge Anthony Vere; Field Hugh J
Antiviral Chemistry & Chemotherapy's current antiviral agents FactFile 2006 (1st edition).
Antiviral chemistry & chemotherapy 2006;17(3):113-66.
-
2006: Torii Takayoshi; Onishi Tomoyuki; Izawa Kunisuke; Maruyama Tokumi; Demizu Yosuke; Neyts Johan; De Clercq Erik
Synthesis of 6-arylthio analogs of 2',3'-dideoxy-3'-fluoroguanosine and their effect against hepatitis B virus replication.
Nucleosides, nucleotides & nucleic acids 2006;25(4-6):655-65.
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2005: Dal Pozzo F; Andrei G; Holy A; Van Den Oord J; Scagliarini A; De Clercq E; Snoeck R
Activities of acyclic nucleoside phosphonates against Orf virus in human and ovine cell monolayers and organotypic ovine raft cultures.
Antimicrobial agents and chemotherapy 2005;49(12):4843-52.
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2005: Rawal Ravindra K; Prabhakar Yenamandra S; Katti S B; De Clercq E
2-(Aryl)-3-furan-2-ylmethyl-thiazolidin-4-ones as selective HIV-RT inhibitors.
Bioorganic & medicinal chemistry 2005;13(24):6771-6.
-
2005: De Clercq Erik; Holý Antonín
Acyclic nucleoside phosphonates: a key class of antiviral drugs.
Nature reviews. Drug discovery 2005;4(11):928-40.
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2005: Lenaerts L; Verbeken E; De Clercq E; Naesens L
Mouse adenovirus type 1 infection in SCID mice: an experimental model for antiviral therapy of systemic adenovirus infections.
Antimicrobial agents and chemotherapy 2005;49(11):4689-99.
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2005: Andrei Graciela; van den Oord Joost; Fiten Pierre; Opdenakker Ghislain; De Wolf-Peeters Chris; De Clercq Erik; Snoeck Robert
Organotypic epithelial raft cultures as a model for evaluating compounds against alphaherpesviruses.
Antimicrobial agents and chemotherapy 2005;49(11):4671-80.
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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.
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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.
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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.
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2005: De Clercq Erik
Recent highlights in the development of new antiviral drugs.
Current opinion in microbiology 2005;8(5):552-60.
-
2005: De Clercq Erik
Potential clinical applications of the CXCR4 antagonist bicyclam AMD3100.
Mini reviews in medicinal chemistry 2005;5(9):805-24.
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2005: Deng Bo-Liang; Hartman Tracy L; Buckheit Robert W; Pannecouque Christophe; De Clercq Erik; Fanwick Phillip E; Cushman Mark
Synthesis, anti-HIV activity, and metabolic stability of new alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry 2005;48(19):6140-55.
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2005: Hatse Sigrid; Princen Katrien; De Clercq Erik; Rosenkilde Mette M; Schwartz Thue W; Hernandez-Abad Pedro E; Skerlj Renato T; Bridger Gary J; Schols Dominique
AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor.
Biochemical pharmacology 2005;70(5):752-61.
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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.
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2005: Scagliarini A; Dal Pozzo F; Gallina L; Guercio A; De Clercq E; Snoeck R; Andrei G
Ovine skin organotypic cultures applied to the ex vivo study of orf virus infection.
Veterinary research communications 2005;29 Suppl 2():245-7.
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2005: Rawal Ravindra K; Solomon V Raja; Prabhakar Yenamandra S; Katti S B; De Clercq E
Synthesis and QSAR studies on thiazolidinones as anti-HIV agents.
Combinatorial chemistry & high throughput screening 2005;8(5):439-43.
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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.
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2005: De Clercq Erik
Antiviral drug discovery and development: where chemistry meets with biomedicine.
Antiviral research 2005;67(2):56-75.
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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.
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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.
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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.
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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.
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2005: Witvrouw Myriam; Fikkert Valery; Hantson Anke; Pannecouque Christophe; O'keefe Barry R; McMahon James; Stamatatos Leonidas; de Clercq Erik; Bolmstedt Anders
Resistance of human immunodeficiency virus type 1 to the high-mannose binding agents cyanovirin N and concanavalin A.
Journal of virology 2005;79(12):7777-84.
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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.
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2005: De Clercq Erik
Emerging anti-HIV drugs.
Expert opinion on emerging drugs 2005;10(2):241-73.
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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.
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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.
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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.
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2005: Daelemans Dirk; Pannecouque Christophe; Pavlakis George N; Tabarrini Oriana; De Clercq Erik
A novel and efficient approach to discriminate between pre- and post-transcription HIV inhibitors.
Molecular pharmacology 2005;67(5):1574-80.
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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.
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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.
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2005: Wu Tongfei; Froeyen Matheus; Kempeneers Veerle; Pannecouque Christophe; Wang Jing; Busson Roger; De Clercq Erik; Herdewijn Piet
Deoxythreosyl phosphonate nucleosides as selective anti-HIV agents.
Journal of the American Chemical Society 2005;127(14):5056-65.
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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.
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2005: González-Díaz Humberto; Cruz-Monteagudo Maykel; Viña Dolores; Santana Lourdes; Uriarte Eugenio; De Clercq Erik
QSAR for anti-RNA-virus activity, synthesis, and assay of anti-RSV carbonucleosides given a unified representation of spectral moments, quadratic, and topologic indices.
Bioorganic & medicinal chemistry letters 2005;15(6):1651-7.
-
2005: De Clercq Erik
New approaches toward anti-HIV chemotherapy.
Journal of medicinal chemistry 2005;48(5):1297-313.
-
2005: Ying C; Holy A; Hocková D; Havlas Z; De Clercq E; Neyts J
Novel acyclic nucleoside phosphonate analogues with potent anti-hepatitis B virus activities.
Antimicrobial agents and chemotherapy 2005;49(3):1177-80.
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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.
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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.
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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.
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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.
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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.
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2005: de Bilderling Georges; Bodart Eddy; Lawson Georges; Tuerlinckx David; Remacle Marc; Naesens Lieve; De Clercq Erik; Snoeck Robert
Successful use of intralesional and intravenous cidofovir in association with indole-3-carbinol in an 8-year-old girl with pulmonary papillomatosis.
Journal of medical virology 2005;75(2):332-5.
-
2005: van Griensven Johan; De Clercq Erik; Debyser Zeger
Hematopoietic stem cell-based gene therapy against HIV infection: promises and caveats.
AIDS reviews 2005;7(1):44-55.
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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.
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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.
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2005: De Bolle Leen; Naesens Lieve; De Clercq Erik
Update on human herpesvirus 6 biology, clinical features, and therapy.
Clinical microbiology reviews 2005;18(1):217-45.
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2005: Fanourgiakis Panagiotis; Georgala Aspasia; Vekemans Marc; Triffet Agnes; De Bruyn Jean-Marc; Duchateau Valerie; Martiat Philippe; De Clercq Erik; Snoeck Robert; Wollants Elke; Rector Annabel; Van Ranst Marc; Aoun Michael
Intravesical instillation of cidofovir in the treatment of hemorrhagic cystitis caused by adenovirus type 11 in a bone marrow transplant recipient.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America 2005;40(1):199-201.
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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.
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2005: De Bolle L; Van Loon J; De Clercq E; Naesens Lieve
Quantitative analysis of human herpesvirus 6 cell tropism.
Journal of medical virology 2005;75(1):76-85.
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2005: De Clercq Erik
(E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU).
Medicinal research reviews 2005;25(1):1-20.
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2005: De Clercq Erik
John Montgomery's legacy: carbocyclic adenosine analogues as SAH hydrolase inhibitors with broad-spectrum antiviral activity.
Nucleosides, nucleotides & nucleic acids 2005;24(10-12):1395-415.
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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.
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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.
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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.
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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.
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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.
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2005: Hantson Anke; Fikkert Valery; Van Remoortel Barbara; Pannecouque Chistophe; Cherepanov Peter; Matthews Barry; Holan George; De Clercq Erik; Vandamme Anne-Mieke; Debyser Zeger; Witvrouw Myriam
Mutations in both env and gag genes are required for HIV-1 resistance to the polysulfonic dendrimer SPL2923, as corroborated by chimeric virus technology.
Antiviral chemistry & chemotherapy 2005;16(4):253-66.
-
2004: De Clercq E
Discovery and development of BVDU (brivudin) as a therapeutic for the treatment of herpes zoster.
Biochemical pharmacology 2004;68(12):2301-15.
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2004: Princen Katrien; Hatse Sigrid; Vermeire Kurt; Aquaro Stefano; De Clercq Erik; Gerlach Lars-Ole; Rosenkilde Mette; Schwartz Thue W; Skerlj Renato; Bridger Gary; Schols Dominique
Inhibition of human immunodeficiency virus replication by a dual CCR5/CXCR4 antagonist.
Journal of virology 2004;78(23):12996-3006.
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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.
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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.
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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.
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2004: Nawrot Barbara; Michalak Olga; De Clercq Erik; Stec Wojciech J
Analogues of acyclic nucleosides derived from tris-(hydroxymethyl)phosphine oxide or bis-(hydroxymethyl)phosphinic acid coupled to DNA nucleobases.
Antiviral chemistry & chemotherapy 2004;15(6):319-28.
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2004: Vermeire Kurt; Princen Katrien; Hatse Sigrid; De Clercq Erik; Dey Kaka; Bell Thomas W; Schols Dominique
CADA, a novel CD4-targeted HIV inhibitor, is synergistic with various anti-HIV drugs in vitro.
AIDS (London, England) 2004;18(16):2115-25.
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2004: Fikkert Valery; Hombrouck Anneleen; Van Remoortel Barbara; De Maeyer Marc; Pannecouque Christophe; De Clercq Erik; Debyser Zeger; Witvrouw Myriam
Multiple mutations in human immunodeficiency virus-1 integrase confer resistance to the clinical trial drug S-1360.
AIDS (London, England) 2004;18(15):2019-28.
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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.
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2004: Tabarrini Oriana; Stevens Miguel; Cecchetti Violetta; Sabatini Stefano; Dell'Uomo Micaela; Manfroni Giuseppe; Palumbo Manlio; Pannecouque Christophe; De Clercq Erik; Fravolini Arnaldo
Structure modifications of 6-aminoquinolones with potent anti-HIV activity.
Journal of medicinal chemistry 2004;47(22):5567-78.
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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.
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2004: Wnuk Stanislaw F; Lewandowska Elzbieta; Sacasa Pablo R; Crain Leigh N; Zhang Jinsong; Borchardt Ronald T; De Clercq Erik
Stereoselective synthesis of sugar-modified enyne analogues of adenosine and uridine. Interaction with S-adenosyl-L-homocysteine hydrolase and antiviral and cytotoxic effects.
Journal of medicinal chemistry 2004;47(21):5251-7.
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2004: De Bolle Leen; Manichanh Chaysavanh; Agut Henri; De Clercq Erik; Naesens Lieve
Human herpesvirus 6 DNA polymerase: enzymatic parameters, sensitivity to ganciclovir and determination of the role of the A961V mutation in HHV-6 ganciclovir resistance.
Antiviral research 2004;64(1):17-25.
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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.
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2004: Hatse Sigrid; Princen Katrien; Liekens Sandra; Vermeire Kurt; De Clercq Erik; Schols Dominique
Fluorescent CXCL12AF647 as a novel probe for nonradioactive CXCL12/CXCR4 cellular interaction studies.
Cytometry. Part A : the journal of the International Society for Analytical Cytology 2004;61(2):178-88.
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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.
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2004: De Clercq Erik
Antiviral research at the Rega Institute (KU leuven), now 50 years old.
Antiviral chemistry & chemotherapy 2004;15(5):223-33.
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2004: De Clercq Erik
Antivirals and antiviral strategies.
Nature reviews. Microbiology 2004;2(9):704-20.
-
2004: De Clercq Erik; Neyts Johan
Therapeutic potential of nucleoside/nucleotide analogues against poxvirus infections.
Reviews in medical virology 2004;14(5):289-300.
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2004: De Clercq Erik
HIV-chemotherapy and -prophylaxis: new drugs, leads and approaches.
The international journal of biochemistry & cell biology 2004;36(9):1800-22.
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2004: Charlier Nathalie; Leyssen Pieter; De Clercq Erik; Neyts Johan
Rodent models for the study of therapy against flavivirus infections.
Antiviral research 2004;63(2):67-77.
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2004: Witvrouw M; Van Maele B; Vercammen J; Hantson A; Engelborghs Y; De Clercq E; Pannecouque C; Debyser Z
Novel inhibitors of HIV-1 integration.
Current drug metabolism 2004;5(4):291-304.
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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.
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2004: Delmas Florence; Avellaneda Antonio; Di Giorgio Carole; Robin Maxime; De Clercq Erik; Timon-David Pierre; Galy Jean-Pierre
Synthesis and antileishmanial activity of (1,3-benzothiazol-2-yl) amino-9-(10H)-acridinone derivatives.
European journal of medicinal chemistry 2004;39(8):685-90.
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2004: Margiotta Nicola; Bergamo Alberta; Sava Gianni; Padovano Giacomo; de Clercq Erik; Natile Giovanni
Antiviral properties and cytotoxic activity of platinum(II) complexes with 1,10-phenanthrolines and acyclovir or penciclovir.
Journal of inorganic biochemistry 2004;98(8):1385-90.
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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.
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2004: Cutrì Christian C C; Garozzo Adriana; Pannecouque Christophe; Castro Angelo; Guerrera Francesco; De Clercq Erik
Isothiazole derivatives as novel HIV replication inhibitors.
Antiviral chemistry & chemotherapy 2004;15(4):201-5.
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2004: Barreca Maria Letizia; Rao Angela; De Luca Laura; Zappalà Maria; Gurnari Cristina; Monforte Pietro; De Clercq Erik; Van Maele Bénédicte; Debyser Zeger; Witvrouw Myriam; Briggs James M; Chimirri Alba
Efficient 3D database screening for novel HIV-1 IN inhibitors.
Journal of chemical information and computer sciences 2004;44(4):1450-5.
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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.
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2004: Charlier Nathalie; Molenkamp Richard; Leyssen Pieter; Paeshuyse Jan; Drosten Christian; Panning Marcus; De Clercq Erik; Bredenbeek Peter J; Neyts Johan
Exchanging the yellow fever virus envelope proteins with Modoc virus prM and E proteins results in a chimeric virus that is neuroinvasive in SCID mice.
Journal of virology 2004;78(14):7418-26.
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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.
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2004: Snoeck R; de Clercq E; Andrei G
[Using antiviral drugs for Orthopoxvirus infections]
Médecine et maladies infectieuses 2004;34 Suppl 1():S48-50.
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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.
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2004: Silvestri Maximilian A; Nagarajan Muthukaman; De Clercq Erik; Pannecouque Christophe; Cushman Mark
Design, synthesis, anti-HIV activities, and metabolic stabilities of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry 2004;47(12):3149-62.
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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.
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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.
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2004: Neyts Johan; Leyssen Pieter; Verbeken Erik; De Clercq Erik
Efficacy of cidofovir in a murine model of disseminated progressive vaccinia.
Antimicrobial agents and chemotherapy 2004;48(6):2267-73.
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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.
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2004: Friedrichs Claudia; Neyts Johan; Gaspar Gabor; De Clercq Erik; Wutzler Peter
Evaluation of antiviral activity against human herpesvirus 8 (HHV-8) and Epstein-Barr virus (EBV) by a quantitative real-time PCR assay.
Antiviral research 2004;62(3):121-3.
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2004: De Clercq Erik
Antiviral drugs in current clinical use.
Journal of clinical virology : the official publication of the Pan American Society for Clinical Virology 2004;30(2):115-33.
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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.
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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.
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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.
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2004: Holm Geoffrey H; Zhang Chengsheng; Gorry Paul R; Peden Keith; Schols Dominique; De Clercq Erik; Gabuzda Dana
Apoptosis of bystander T cells induced by human immunodeficiency virus type 1 with increased envelope/receptor affinity and coreceptor binding site exposure.
Journal of virology 2004;78(9):4541-51.
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2004: Andrei G; De Clercq E; Snoeck R
In vitro selection of drug-resistant varicella-zoster virus (VZV) mutants (OKA strain): differences between acyclovir and penciclovir?
Antiviral research 2004;61(3):181-7.
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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.
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2004: van Griensven Johan; Zhan Xiaojing; Van Maele Bénédicte; Pluymers Wim; Michiels Martine; De Clercq Erik; Cherepanov Peter; Debyser Zeger
Expression of HIV-1 integrase in CEM cells inhibits HIV-1 replication.
The journal of gene medicine 2004;6(3):268-77.
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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.
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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.
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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.
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2004: Witvrouw Myriam; Pannecouque Christophe; Switzer William M; Folks Thomas M; De Clercq Erik; Heneine Walid
Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis.
Antiviral therapy 2004;9(1):57-65.
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2004: De Bolle Leen; Hatse Sigrid; Verbeken Erik; De Clercq Erik; Naesens Lieve
Human herpesvirus 6 infection arrests cord blood mononuclear cells in G(2) phase of the cell cycle.
FEBS letters 2004;560(1-3):25-9.
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2004: Anastasi Carole; Hantz Olivier; De Clercq Erik; Pannecouque Christophe; Clayette Pascal; Dereuddre-Bosquet Nathalie; Dormont Dominique; Gondois-Rey Françoise; Hirsch Ivan; Kraus Jean-Louis
Potent nonclassical nucleoside antiviral drugs based on the N,N-diarylformamidine concept.
Journal of medicinal chemistry 2004;47(5):1183-92.
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2004: Padalko Elizaveta; Verbeken Erik; De Clercq Erik; Neyts Johan
Inhibition of coxsackie B3 virus induced myocarditis in mice by 2-(3,4-dichlorophenoxy)-5-nitrobenzonitrile.
Journal of medical virology 2004;72(2):263-7.
-
2004: De Clercq Erik
Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future.
Chemistry & biodiversity 2004;1(1):44-64.
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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.
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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.
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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.
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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: De Bolle Leen; Andrei Graciela; Snoeck Robert; Zhang Ying; Van Lommel Alfons; Otto Michael; Bousseau Anne; Roy Christine; De Clercq Erik; Naesens Lieve
Potent, selective and cell-mediated inhibition of human herpesvirus 6 at an early stage of viral replication by the non-nucleoside compound CMV423.
Biochemical pharmacology 2004;67(2):325-36.
-
2004: Fonseca Tatiana; Gigante Bárbara; Marques M Matilde; Gilchrist Thomas L; De Clercq Erik
Synthesis and antiviral evaluation of benzimidazoles, quinoxalines and indoles from dehydroabietic acid.
Bioorganic & medicinal chemistry 2004;12(1):103-12.
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2004: Padalko Elizaveta; Nuyens Dieter; De Palma Armando; Verbeken Erik; Aerts Joeri L; De Clercq Erik; Carmeliet Peter; Neyts Johan
The interferon inducer ampligen [poly(I)-poly(C12U)] markedly protects mice against coxsackie B3 virus-induced myocarditis.
Antimicrobial agents and chemotherapy 2004;48(1):267-74.
-
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: Sinha Sarika; Srivastava Richa; De Clercq Erik; Singh Ramendra K
Synthesis and antiviral properties of arabino and ribonucleosides of 1,3-dideazaadenine, 4-nitro-1,3-dideazapurine and diketopiperazine.
Nucleosides, nucleotides & nucleic acids 2004;23(12):1815-24.
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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: Raic-Malic Silvana; Johayem Anass; Ametamey Simon M; Batinac Sanja; De Clercq Erik; Folkers Gerd; Scapozza Leonardo
Synthesis, 18F-radiolabelling and biological evaluations of C-6 alkylated pyrimidine nucleoside analogues.
Nucleosides, nucleotides & nucleic acids 2004;23(11):1707-21.
-
2004: Taourirte M; Mohamed L Ait; Rochdi A; Vasseur J J; Fernández S; Ferrero M; Gotor V; Pannecouque C; De Clercq E; Lazrek H B
Chemoenzymatic syntheses of homo- and heterodimers of AZT and d4T, and evaluation of their anti-HIV activity.
Nucleosides, nucleotides & nucleic acids 2004;23(4):701-14.
-
2004: Princen Katrien; Hatse Sigrid; Vermeire Kurt; De Clercq Erik; Schols Dominique
Establishment of a novel CCR5 and CXCR4 expressing CD4+ cell line which is highly sensitive to HIV and suitable for high-throughput evaluation of CCR5 and CXCR4 antagonists.
Retrovirology 2004;1():2.
-
2004: De Clercq Erik
Nucleoside analogues exerting antiviral activity through a non-nucleoside mechanism.
Nucleosides, nucleotides & nucleic acids 2004;23(1-2):457-70.
-
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: Princen Katrien; Hatse Sigrid; Vermeire Kurt; Bridger Gary J; Skerlj Renato T; De Clercq Erik; Schols Dominique
The antiviral activity of the CXCR4 antagonist AMD3100 is independent of the cytokine-induced CXCR4/HIV coreceptor expression level.
AIDS research and human retroviruses 2003;19(12):1135-9.
-
2003: Padalko Elizaveta; Verbeken Erik; Matthys Patrick; Aerts Joeri L; De Clercq Erik; Neyts Johan
Mycophenolate mofetil inhibits the development of Coxsackie B3-virus-induced myocarditis in mice.
BMC microbiology 2003;3():25.
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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: 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: Stamatiou George; Foscolos George B; Fytas George; Kolocouris Antonios; Kolocouris Nicolas; Pannecouque Christophe; Witvrouw Myriam; Padalko Elizaveta; Neyts Johan; De Clercq Erik
Heterocyclic rimantadine analogues with antiviral activity.
Bioorganic & medicinal chemistry 2003;11(24):5485-92.
-
2003: Witvrouw Myriam; Pannecouque Christophe; Fikkert Valery; Hantson Anke; Van Remoortel Barbara; Hezareh Marjan; De Clercq Erik; Brown Stephen J
Potent and selective inhibition of HIV and SIV by prostratin interacting with viral entry.
Antiviral chemistry & chemotherapy 2003;14(6):321-8.
-
2003: Zhao Qian; Lu Hong; Schols Dominique; De Clercq Erik; Jiang Shibo
Development of a cell-based enzyme-linked immunosorbent assay for high-throughput screening of HIV type 1 entry inhibitors targeting the coreceptor CXCR4.
AIDS research and human retroviruses 2003;19(11):947-55.
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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.
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2003: Fikkert Valery; Van Maele Bénédicte; Vercammen Jo; Hantson Anke; Van Remoortel Barbara; Michiels Martine; Gurnari Cristina; Pannecouque Christophe; De Maeyer Marc; Engelborghs Yves; De Clercq Erik; Debyser Zeger; Witvrouw Myriam
Development of resistance against diketo derivatives of human immunodeficiency virus type 1 by progressive accumulation of integrase mutations.
Journal of virology 2003;77(21):11459-70.
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2003: Lavandera Iván; Fernández Susana; Ferrero Miguel; De Clercq Erik; Gotor Vicente
Synthesis, protonation behavior, conformational analysis, and regioselective enzymatic acylation of the novel diamino analogue of (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU).
Nucleosides, nucleotides & nucleic acids 2003;22(10):1939-52.
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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: De Clercq Erik
Clinical potential of the acyclic nucleoside phosphonates cidofovir, adefovir, and tenofovir in treatment of DNA virus and retrovirus infections.
Clinical microbiology reviews 2003;16(4):569-96.
-
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: Ying Chunxiao; De Clercq Erik; Neyts Johan
Selective inhibition of hepatitis B virus replication by RNA interference.
Biochemical and biophysical research communications 2003;309(2):482-4.
-
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.
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2003: Anastasi Carole; Vlieghe Patrick; Hantz Olivier; Schorr Olivier; Pannecouque Christophe; Witvrouw Myriam; De Clercq Erik; Clayette Pascal; Dereuddre-Bosquet Nathalie; Dormont Dominique; Gondois-Rey Françoise; Hirsch Ivan; Kraus Jean-Louis
Are 5'-O-carbamate-2',3'-dideoxythiacytidine new anti-HIV and anti-HBV nucleoside drugs or prodrugs?
Bioorganic & medicinal chemistry letters 2003;13(15):2459-63.
-
2003: Maertens Goedele; Cherepanov Peter; Pluymers Wim; Busschots Katrien; De Clercq Erik; Debyser Zeger; Engelborghs Yves
LEDGF/p75 is essential for nuclear and chromosomal targeting of HIV-1 integrase in human cells.
The Journal of biological chemistry 2003;278(35):33528-39.
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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.
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2003: Leyssen Pieter; Croes Romaric; Rau Philipp; Heiland Sabine; Verbeken Erik; Sciot Raphael; Paeshuyse Jan; Charlier Nathalie; De Clercq Erik; Meyding-Lamadé Uta; Neyts Johan
Acute encephalitis, a poliomyelitis-like syndrome and neurological sequelae in a hamster model for flavivirus infections.
Brain pathology (Zurich, Switzerland) 2003;13(3):279-90.
-
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.
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2003: Hatse Sigrid; Princen Katrien; Vermeire Kurt; Gerlach Lars-Ole; Rosenkilde Mette M; Schwartz Thue W; Bridger Gary; De Clercq Erik; Schols Dominique
Mutations at the CXCR4 interaction sites for AMD3100 influence anti-CXCR4 antibody binding and HIV-1 entry.
FEBS letters 2003;546(2-3):300-6.
-
2003: De Clercq Erik
The bicyclam AMD3100 story.
Nature reviews. Drug discovery 2003;2(7):581-7.
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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.
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2003: Willey Samantha J; Reeves Jacqueline D; Hudson Richard; Miyake Koichi; Dejucq Nathalie; Schols Dominique; De Clercq Erik; Bell Jeanne; McKnight Aine; Clapham Paul R
Identification of a subset of human immunodeficiency virus type 1 (HIV-1), HIV-2, and simian immunodeficiency virus strains able to exploit an alternative coreceptor on untransformed human brain and lymphoid cells.
Journal of virology 2003;77(11):6138-52.
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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.
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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.
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2003: Moukha-chafiq O; Taha M L; Mouma A; Lazrek H B; Vasseur J J; De Clercq E
Synthesis and biological evaluation of some acyclic 4,6-disubstituted 1H-pyrazolo[3,4-d]pyrimidine nucleosides.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):967-72.
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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: Van Aerschot A; Schepers G; Busson R; Neyts J; De Clercq E; Herdewijn P
Synthesis and antiviral evaluation of ribavirin congeners containing a hexitol moiety.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):849-51.
-
2003: Gu Ping; Morral Jordi; Wang Jing; Rozenski Jef; Busson Roger; Van Aerschot Arthur; De Clercq Erik; Herdewijn Piet
Synthesis and biological evaluation of a series of new cyclohexenyl nucleosides.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):845-7.
-
2003: Lavandera Iván; Fernández Susana; Ferrero Miguel; De Clercq Erik; Gotor Vicente
Synthesis and antiviral activity assay of novel (E)-3',5'-diamino-5-(2-bromovinyl)-2',3',5'-trideoxyuridine.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):833-6.
-
2003: Ait Mohamed L; Taourirte M; Rochdi A; Lazrek H B; Vasseur J J; Engels J W; Pannecouque C; De Clercq E
Synthesis of new homo and heterodimers of 2',3'-dideoxyinosine (ddI) using ester linkages.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):829-31.
-
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: 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: Terán C; Santana L; Uriarte E; Viña D; De Clercq E
Purine derivatives of 1,2-disubstituted cyclohexane analogues of nucleosides.
Nucleosides, nucleotides & nucleic acids 2003;22(5-8):787-9.
-
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.
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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: Zoidis Grigoris; Kolocouris Nicolas; Foscolos George B; Kolocouris Antonios; Fytas George; Karayannis P; Padalko Elizaveta; Neyts Johan; De Clercq Erik
Are the 2-isomers of the drug rimantadine active anti-influenza A agents?
Antiviral chemistry & chemotherapy 2003;14(3):153-64.
-
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: Stylianakis Ioannis; Kolocouris Antonios; Kolocouris Nicolas; Fytas George; Foscolos George B; Padalko Elizaveta; Neyts Johan; De Clercq Erik
Spiro[pyrrolidine-2,2'-adamantanes]: synthesis, anti-influenza virus activity and conformational properties.
Bioorganic & medicinal chemistry letters 2003;13(10):1699-703.
-
2003: Jekle Andreas; Keppler Oliver T; De Clercq Erik; Schols Dominique; Weinstein Mark; Goldsmith Mark A
In vivo evolution of human immunodeficiency virus type 1 toward increased pathogenicity through CXCR4-mediated killing of uninfected CD4 T cells.
Journal of virology 2003;77(10):5846-54.
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2003: Suzutani Tatsuo; Ishioka Ken; De Clercq Erik; Ishibashi Kei; Kaneko Hisatoshi; Kira Toshihiko; Hashimoto Koh-Ichi; Ogasawara Masahiro; Ohtani Katsuki; Wakamiya Nobutaka; Saijo Masayuki
Differential mutation patterns in thymidine kinase and DNA polymerase genes of herpes simplex virus type 1 clones passaged in the presence of acyclovir or penciclovir.
Antimicrobial agents and chemotherapy 2003;47(5):1707-13.
-
2003: De Clercq Erik
New inhibitors of human cytomegalovirus (HCMV) on the horizon.
The Journal of antimicrobial chemotherapy 2003;51(5):1079-83.
-
2003: De Clercq Erik
Highly potent and selective inhibition of varicella-zoster virus replication by bicyclic furo[2,3-d]pyrimidine nucleoside analogues.
Medicinal research reviews 2003;23(3):253-74.
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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.
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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: Van Maele Bénédicte; De Rijck Jan; De Clercq Erik; Debyser Zeger
Impact of the central polypurine tract on the kinetics of human immunodeficiency virus type 1 vector transduction.
Journal of virology 2003;77(8):4685-94.
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2003: Barreca Maria Letizia; Chimirri Alba; De Clercq Erik; De Luca Laura; Monforte Anna-Maria; Monforte Pietro; Rao Angela; Zappalà Maria
Anti-HIV agents: design and discovery of new potent RT inhibitors.
Farmaco (Società chimica italiana : 1989) 2003;58(3):259-63.
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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: Okamoto Mika; Wang Xin; Debyser Zeger; De Clercq Erik; Baba Masanori
Establishment of an in vitro assay system mimicking human immunodeficiency virus type 1-induced neural cell death and evaluation of inhibitors thereof.
Journal of virological methods 2003;108(2):195-203.
-
2003: Charlier Nathalie; Molenkamp Richard; Leyssen Pieter; Vandamme Anne Mieke; De Clercq Erik; Bredenbeek Peter; Neyts Johan
A rapid and convenient variant of fusion-PCR to construct chimeric flaviviruses.
Journal of virological methods 2003;108(1):67-74.
-
2003: Armand-Ugón Mercedes; Quiñones-Mateu Miguel E; Gutiérez Arantxa; Barretina Jordi; Blanco Julià; Schols Dominique; De Clercq Erik; Clotet Bonaventura; Esté José A
Reduced fitness of HIV-1 resistant to CXCR4 antagonists.
Antiviral therapy 2003;8(1):1-8.
-
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.
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2003: Leyssen Pieter; Paeshuyse Jan; Charlier Nathalie; Van Lommel Alfons; Drosten Christian; De Clercq Erik; Neyts Johan
Impact of direct virus-induced neuronal dysfunction and immunological damage on the progression of flavivirus (Modoc) encephalitis in a murine model.
Journal of neurovirology 2003;9(1):69-78.
-
2003: Rao Angela; Carbone Anna; Chimirri Alba; De Clercq Erik; Monforte Anna Maria; Monforte Pietro; Pannecouque Christophe; Zappalà Maria
Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-ones.
Farmaco (Società chimica italiana : 1989) 2003;58(2):115-20.
-
2003: Leyssen Pieter; Drosten Christian; Paning Marcus; Charlier Nathalie; Paeshuyse Jan; De Clercq Erik; Neyts Johan
Interferons, interferon inducers, and interferon-ribavirin in treatment of flavivirus-induced encephalitis in mice.
Antimicrobial agents and chemotherapy 2003;47(2):777-82.
-
2003: Gu Ping; Morral Jordi; Wang Jing; Rozenski Jef; Busson Roger; Van Aerschot Arthur; De Clercq Erik; Herdewijn Piet
Synthesis and antiviral activity of a series of new cyclohexenyl nucleosides.
Antiviral chemistry & chemotherapy 2003;14(1):31-7.
-
2003: Van Aerschot Arthur; Schepers Guy; Busson Roger; Rozenski Jef; Neyts Johan; De Clercq Erik; Herdewijn Piet
Ribavirin derivatives with a hexitol moiety: synthesis and antiviral evaluation.
Antiviral chemistry & chemotherapy 2003;14(1):23-30.
-
2003: Neyts Johan; De Clercq Erik
Therapy and short-term prophylaxis of poxvirus infections: historical background and perspectives.
Antiviral research 2003;57(1-2):25-33.
-
2003: Princen Katrien; Hatse Sigrid; Vermeire Kurt; De Clercq Erik; Schols Dominique
Evaluation of SDF-1/CXCR4-induced Ca2+ signaling by fluorometric imaging plate reader (FLIPR) and flow cytometry.
Cytometry. Part A : the journal of the International Society for Analytical Cytology 2003;51(1):35-45.
-
2003: Vermeire Kurt; Bell Thomas W; Choi Heung-Jin; Jin Qi; Samala Meinrado F; Sodoma Andrej; De Clercq Erik; Schols Dominique
The Anti-HIV potency of cyclotriazadisulfonamide analogs is directly correlated with their ability to down-modulate the CD4 receptor.
Molecular pharmacology 2003;63(1):203-10.
-
2003: Cherepanov Peter; Maertens Goedele; Proost Paul; Devreese Bart; Van Beeumen Jozef; Engelborghs Yves; De Clercq Erik; Debyser Zeger
HIV-1 integrase forms stable tetramers and associates with LEDGF/p75 protein in human cells.
The Journal of biological chemistry 2003;278(1):372-81.
-
2003: Hatse S; Bridger G; de Clercq E; Schols D
X4 HIV-1 induces neuroblastoma cell death by interference with CXCL12/CXCR4 interaction.
Cellular and molecular biology (Noisy-le-Grand, France) 2003;49 Online Pub():OL443-52.
-
2003: Leyssen P; Charlier N; Paeshuyse J; De Clercq E; Neyts J
Prospects for antiviral therapy.
Advances in virus research 2003;61():511-53.
-
2003: Mager Peter P; De Clercq Erik; Froeyen Matheus; Reinhardt Robert
Interactions of the dimeric triad of HIV-1 aspartyl protease with inhibitors.
Drug design and discovery 2003;18(2-3):53-64.
-
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: Fikkert Valery; Cherepanov Peter; Van Laethem Kristel; Hantson Anke; Van Remoortel Barbara; Pannecouque Christophe; De Clercq Erik; Debyser Zeger; Vandamme Anne-Mieke; Witvrouw Myriam
env chimeric virus technology for evaluating human immunodeficiency virus susceptibility to entry inhibitors.
Antimicrobial agents and chemotherapy 2002;46(12):3954-62.
-
2002: Saijo Masayuki; Suzutani Tatsuo; De Clercq Erik; Niikura Masahiro; Maeda Akihiko; Morikawa Shigeru; Kurane Ichiro
Genotypic and phenotypic characterization of the thymidine kinase of ACV-resistant HSV-1 derived from an acyclovir-sensitive herpes simplex virus type 1 strain.
Antiviral research 2002;56(3):253-62.
-
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.
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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.
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2002: Snoeck R; Holý A; Dewolf-Peeters C; Van Den Oord J; De Clercq E; Andrei G
Antivaccinia activities of acyclic nucleoside phosphonate derivatives in epithelial cells and organotypic cultures.
Antimicrobial agents and chemotherapy 2002;46(11):3356-61.
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2002: De Clercq Erik
New anti-HIV agents and targets.
Medicinal research reviews 2002;22(6):531-65.
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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.
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2002: Vermeire Kurt; Zhang Ying; Princen Katrien; Hatse Sigrid; Samala Meinrado F; Dey Kaka; Choi Heung-Jin; Ahn Youngmi; Sodoma Andrej; Snoeck Robert; Andrei Graciela; De Clercq Erik; Bell Thomas W; Schols Dominique
CADA inhibits human immunodeficiency virus and human herpesvirus 7 replication by down-modulation of the cellular CD4 receptor.
Virology 2002;302(2):342-53.
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2002: Rao Angela; Chimirri Alba; De Clercq Erik; Monforte Anna Maria; Monforte Pietro; Pannecouque Christophe; Zappalà Maria
Synthesis and anti-hIV activity of 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazole structurally-related 1,2-substituted benzimidazoles.
Farmaco (Società chimica italiana : 1989) 2002;57(10):819-23.
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2002: Daelemans Dirk; Afonina Elena; Nilsson Jakob; Werner Gudrun; Kjems Jorgen; De Clercq Erik; Pavlakis George N; Vandamme Anne-Mieke
A synthetic HIV-1 Rev inhibitor interfering with the CRM1-mediated nuclear export.
Proceedings of the National Academy of Sciences of the United States of America 2002;99(22):14440-5.
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2002: De Clercq Erik
Cidofovir in the therapy and short-term prophylaxis of poxvirus infections.
Trends in pharmacological sciences 2002;23(10):456-8.
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2002: Gáspár Gábor; De Clercq Erik; Neyts Johan
Gammaherpesviruses encode functional dihydrofolate reductase activity.
Biochemical and biophysical research communications 2002;297(4):756-9.
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2002: Gáspár Gábor; De Clercq Erik; Neyts Johan
Human herpesvirus 8 gene encodes a functional thymidylate synthase.
Journal of virology 2002;76(20):10530-2.
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2002: Pluymers Wim; Pais Godwin; Van Maele Bénédicte; Pannecouque Christophe; Fikkert Valery; Burke Terrence R; De Clercq Erik; Witvrouw Myriam; Neamati Nouri; Debyser Zeger
Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives.
Antimicrobial agents and chemotherapy 2002;46(10):3292-7.
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2002: Garuti Laura; Roberti Marinella; De Clercq Erik
Synthesis and antiviral/antiproliferative activity of some N-sulphonylbenzimidazoles.
Bioorganic & medicinal chemistry letters 2002;12(19):2707-10.
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2002: Vercammen Jo; Maertens Goedele; Gerard Melanie; De Clercq Erik; Debyser Zeger; Engelborghs Yves
DNA-induced polymerization of HIV-1 integrase analyzed with fluorescence fluctuation spectroscopy.
The Journal of biological chemistry 2002;277(41):38045-52.
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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.
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2002: Rao Angela; Carbone Anna; Chimirri Alba; De Clercq Erik; Monforte Anna Maria; Monforte Pietro; Pannecouque Christophe; Zappalà Maria
Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-(thi)one derivatives.
Farmaco (Società chimica italiana : 1989) 2002;57(9):747-51.
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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.
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2002: Hatse Sigrid; Princen Katrien; Bridger Gary; De Clercq Erik; Schols Dominique
Chemokine receptor inhibition by AMD3100 is strictly confined to CXCR4.
FEBS letters 2002;527(1-3):255-62.
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2002: Saijo Masayuki; Yasuda Yukiharu; Yabe Hiromasa; Kato Shunichi; Suzutani Tatsuo; De Clercq Erik; Niikura Masahiro; Maeda Akihiko; Kurane Ichiro; Morikawa Shigeru
Bone marrow transplantation in a child with Wiskott-Aldrich syndrome latently infected with acyclovir-resistant (ACV(r)) herpes simplex virus type 1: emergence of foscarnet-resistant virus originating from the ACV(r) virus.
Journal of medical virology 2002;68(1):99-104.
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2002: Snoeck Robert; Andrei Graciela; Bodaghi Bahram; Lagneaux Laurence; Daelemans Dirk; de Clercq Erik; Neyts Johan; Schols Dominique; Naesens Lieve; Michelson Susan; Bron Dominique; Otto Michael J; Bousseau Anne; Nemecek Conception; Roy Christine
2-Chloro-3-pyridin-3-yl-5,6,7,8-tetrahydroindolizine-1-carboxamide (CMV423), a new lead compound for the treatment of human cytomegalovirus infections.
Antiviral research 2002;55(3):413-24.
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2002: Neyts Johan; Verbeken Erik; De Clercq Erik
Effect of 5-iodo-2'-deoxyuridine on vaccinia virus (orthopoxvirus) infections in mice.
Antimicrobial agents and chemotherapy 2002;46(9):2842-7.
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2002: De Bolle Leen; Michel Detlef; Mertens Thomas; Manichanh Chaysavanh; Agut Henri; De Clercq Erik; Naesens Lieve
Role of the human herpesvirus 6 u69-encoded kinase in the phosphorylation of ganciclovir.
Molecular pharmacology 2002;62(3):714-21.
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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.
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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.
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2002: Charlier Nathalie; Leyssen Pieter; Paeshuyse Jan; Drosten Christian; Schmitz Herbert; Van Lommel Alfons; De Clercq Erik; Neyts Johan
Infection of SCID mice with Montana Myotis leukoencephalitis virus as a model for flavivirus encephalitis.
The Journal of general virology 2002;83(Pt 8):1887-96.
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2002: Charlier Nathalie; Leyssen Pieter; Pleij Cornelis W A; Lemey Philippe; Billoir Frédérique; Van Laethem Kristel; Vandamme Anne-Mieke; De Clercq Erik; de Lamballerie Xavier; Neyts Johan
Complete genome sequence of Montana Myotis leukoencephalitis virus, phylogenetic analysis and comparative study of the 3' untranslated region of flaviviruses with no known vector.
The Journal of general virology 2002;83(Pt 8):1875-85.
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2002: van Gelder J; Deferme S; Naesens L; De Clercq E; van den Mooter G; Kinget R; Augustijns P
Intestinal absorption enhancement of the ester prodrug tenofovir disoproxil fumarate through modulation of the biochemical barrier by defined ester mixtures.
Drug metabolism and disposition: the biological fate of chemicals 2002;30(8):924-30.
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2002: Van Vaerenbergh Kristien; De Geest Sabina; Derdelinckx Inge; Bobbaers Herman; Carbonez An; Deschamps Ann; De Graeve Veerle; De Saar Veerle; Ceunen Helga; De Smet Koen; Maes Bart; Peetermans Willy; Schrooten Yoeri; Desmyter Jan; De Clercq Erik; Van Ranst Marc; Van Wijngaerden Eric; Vandamme Anne-Mieke
A combination of poor adherence and a low baseline susceptibility score is highly predictive for HAART failure.
Antiviral chemistry & chemotherapy 2002;13(4):231-40.
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2002: Pannecouque Christophe; Pluymers Wim; Van Maele Bénédicte; Tetz Victor; Cherepanov Peter; De Clercq Erik; Witvrouw Myriam; Debyser Zeger
New class of HIV integrase inhibitors that block viral replication in cell culture.
Current biology : CB 2002;12(14):1169-77.
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2002: Simonart Thierry; Boelaert Johan R; Andrei Graciela; van den Oord Joost J; Degraef Chantale; Hermans Philippe; Noel Jean-Christophe; Van Vooren Jean-Paul; Heenen Michel; De Clercq Erik; Snoeck Robert
Desferrioxamine enhances AIDS-associated Kaposi's sarcoma tumor development in a xenograft model.
International journal of cancer. Journal international du cancer 2002;100(2):140-3.
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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.
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2002: De Clercq Erik
New developments in anti-HIV chemotherapy.
Biochimica et biophysica acta 2002;1587(2-3):258-75.
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2002: De Clercq Erik
Cidofovir in the treatment of poxvirus infections.
Antiviral research 2002;55(1):1-13.
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2002: Jekle Andreas; Schramm Birgit; Jayakumar Prerana; Trautner Verena; Schols Dominique; De Clercq Erik; Mills John; Crowe Suzanne M; Goldsmith Mark A
Coreceptor phenotype of natural human immunodeficiency virus with nef deleted evolves in vivo, leading to increased virulence.
Journal of virology 2002;76(14):6966-73.
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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.
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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.
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2002: Wnuk Stanislaw F; Ro Bong-Oh; Valdez Carlos A; Lewandowska Elzbieta; Valdez Neida X; Sacasa Pablo R; Yin Dan; Zhang Jinsong; Borchardt Ronald T; De Clercq Erik
Sugar-modified conjugated diene analogues of adenosine and uridine: synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects.
Journal of medicinal chemistry 2002;45(12):2651-8.
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2002: Salido Sofía; Altarejos Joaquín; Nogueras Manuel; Sánchez Adolfo; Pannecouque Christophe; Witvrouw Myriam; De Clercq Erik
Chemical studies of essential oils of Juniperus oxycedrus ssp. badia.
Journal of ethnopharmacology 2002;81(1):129-34.
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2002: Stragier Ilse; Snoeck Robert; De Clercq Erik; Van Den Oord Joost J; Van Ranst Marc; De Greef Hugo
Local treatment of HPV-induced skin lesions by Cidofovir.
Journal of medical virology 2002;67(2):241-5.
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2002: Bergstrom Donald E; Lin Xiaoping; Wood Troy D; Witvrouw Myriam; Ikeda Satoru; Andrei Graciela; Snoeck Robert; Schols Dominique; De Clercq Erik
Polysulfonates derived from metal thiolate complexes as inhibitors of HIV-1 and various other enveloped viruses in vitro.
Antiviral chemistry & chemotherapy 2002;13(3):185-95.
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2002: Ying C; Van Pelt J F; Van Lommel A; Van Ranst M; Leyssen P; De Clercq E; Neyts J
Sulphated and sulphonated polymers inhibit the initial interaction of hepatitis B virus with hepatocytes.
Antiviral chemistry & chemotherapy 2002;13(3):157-64.
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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.
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2002: Hillenkamp Jost; Reinhard Thomas; Ross Rudolf S; Böhringer Daniel; Cartsburg Olaf; Roggendorf Michael; De Clercq Erik; Godehardt Erhard; Sundmacher Rainer
The effects of cidofovir 1% with and without cyclosporin a 1% as a topical treatment of acute adenoviral keratoconjunctivitis: a controlled clinical pilot study.
Ophthalmology 2002;109(5):845-50.
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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.
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2002: De Clercq E
Highlights in the development of new antiviral agents.
Mini reviews in medicinal chemistry 2002;2(2):163-75.
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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.
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2002: Van Vaerenbergh K; Harrer T; Schmit J-C; Carbonez A; Fontaine E; Kurowski M; Grünke M; Löw P; Rascu A; Schmidt B; Schmitt M; Thoelen I; Walter H; Van Laethem K; Van Ranst M; Desmyter J; De Clercq E; Vandamme A-M
Initiation of HAART in drug-naive HIV type 1 patients prevents viral breakthrough for a median period of 35.5 months in 60% of the patients.
AIDS research and human retroviruses 2002;18(6):419-26.
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2002: Snoeck Joke; Van Dooren Sonia; Van Laethem Kristel; Derdelinckx Inge; Van Wijngaerden Eric; De Clercq Erik; Vandamme Anne-Mieke
Prevalence and origin of HIV-1 group M subtypes among patients attending a Belgian hospital in 1999.
Virus research 2002;85(1):95-107.
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2002: Simonart Thierry; Boelaert Johan R; Mosselmans Roger; Andrei Graciela; Noel Jean-Christophe; De Clercq Erik; Snoeck Robert
Antiproliferative and apoptotic effects of iron chelators on human cervical carcinoma cells.
Gynecologic oncology 2002;85(1):95-102.
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2002: Naif Hassan M; Cunningham Anthony L; Alali Mohammed; Li Shan; Nasr Najla; Buhler Marc M; Schols Dominique; de Clercq Erik; Stewart Graeme
A human immunodeficiency virus type 1 isolate from an infected person homozygous for CCR5Delta32 exhibits dual tropism by infecting macrophages and MT2 cells via CXCR4.
Journal of virology 2002;76(7):3114-24.
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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.
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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.
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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.
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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.
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2002: Kritsanida Marina; Mouroutsou Anastasia; Marakos Panagiotis; Pouli Nicole; Papakonstantinou-Garoufalias Spyroula; Pannecouque Christophe; Witvrouw Myriam; De Clercq Erik
Synthesis and antiviral activity evaluation of some new 6-substituted 3-(1-adamantyl)-1,2,4-triazolo[3,4-b][1,3,4]thiadiazoles.
Farmaco (Società chimica italiana : 1989) 2002;57(3):253-7.
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2002: Vlieghe Patrick; Clerc Thierry; Pannecouque Christophe; Witvrouw Myriam; De Clercq Erik; Salles Jean-Pierre; Kraus Jean-Louis
Synthesis of new covalently bound kappa-carrageenan-AZT conjugates with improved anti-HIV activities.
Journal of medicinal chemistry 2002;45(6):1275-83.
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2002: Kolocouris Antonios; Dimas Kostas; Pannecouque Christophe; Witvrouw Myriam; Foscolos George B; Stamatiou George; Fytas George; Zoidis Grigoris; Kolocouris Nicolas; Andrei Graciela; Snoeck Robert; De Clercq Erik
New 2-(1-adamantylcarbonyl)pyridine and 1-acetyladamantane thiosemicarbazones-thiocarbonohydrazones: cell growth inhibitory, antiviral and antimicrobial activity evaluation.
Bioorganic & medicinal chemistry letters 2002;12(5):723-7.
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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.
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2002: Snoeck Robert; De Clercq Erik
New treatments for genital herpes.
Current opinion in infectious diseases 2002;15(1):49-55.
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2002: Leyssen Pieter; Charlier Nathalie; Lemey Philippe; Billoir Frédérique; Vandamme Anne-Mieke; De Clercq Erik; de Lamballerie Xavier; Neyts Johan
Complete genome sequence, taxonomic assignment, and comparative analysis of the untranslated regions of the Modoc virus, a flavivirus with no known vector.
Virology 2002;293(1):125-40.
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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.
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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.
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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.
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2002: Debyser Zeger; Cherepanov Peter; Van Maele Bénédicte; De Clercq Erik; Witvrouw Myriam
In search of authentic inhibitors of HIV-1 integration.
Antiviral chemistry & chemotherapy 2002;13(1):1-15.
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2002: De Clercq Erik
Strategies in the design of antiviral drugs.
Nature reviews. Drug discovery 2002;1(1):13-25.
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2002: Moukha-chafiq Omar; Taha Mohamed Labd; Lazrek Hassan Bihi; Vasseur Jean-Jacques; Pannecouque Christophe; Witvrouw Myriam; De Clercq Erik
Synthesis and biological activity of some 4-substituted 1-[1-(2,3-dihydroxy-1-propoxy)methyl-1,2,3-triazol-(4 & 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines.
Farmaco (Società chimica italiana : 1989) 2002;57(1):27-32.
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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.
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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.
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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.
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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.
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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.
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2002: Moukha-chafiq O; Taha M L; Lazrek H B; Vasseur J J; De Clercq E
Synthesis and biological evaluation of some acyclic alpha-(1H-pyrazolo-[3,4-d]pyrimidin-4-yl)thioalkylamide nucleosides.
Nucleosides, nucleotides & nucleic acids 2002;21(2):165-76.
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2001: Lazrek H B; Taourirte M; Oulih T; Barascut J L; Imbach J L; Pannecouque C; Witrouw M; De Clercq E
Synthesis and anti-HIV activity of new modified 1,2,3-triazole acyclonucleosides.
Nucleosides, nucleotides & nucleic acids 2001;20(12):1949-60.
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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.
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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.
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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.
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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.
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2001: Meerbach A; Neyts J; Balzarini J; Helbig B; De Clercq E; Wutzler P
In vitro activity of polyhydroxycarboxylates against herpesviruses and HIV.
Antiviral chemistry & chemotherapy 2001;12(6):337-45.
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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.
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2001: De Clercq E; Naesens L; De Bolle L; Schols D; Zhang Y; Neyts J
Antiviral agents active against human herpesviruses HHV-6, HHV-7 and HHV-8.
Reviews in medical virology 2001;11(6):381-95.
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2001: Golankiewicz B; Ostrowski T; Goslinski T; Januszczyk P; Zeidler J; Baranowski D; de Clercq E
Fluorescent tricyclic analogues of acyclovir and ganciclovir. A structure-antiviral activity study.
Journal of medicinal chemistry 2001;44(24):4284-7.
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2001: Fontaine E; Riva C; Peeters M; Schmit J C; Delaporte E; Van Laethem K; Van Vaerenbergh K; Snoeck J; Van Wijngaerden E; De Clercq E; Van Ranst M; Vandamme A M
Evaluation of two commercial kits for the detection of genotypic drug resistance on a panel of HIV type 1 subtypes A through J.
Journal of acquired immune deficiency syndromes (1999) 2001;28(3):254-8.
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2001: Casimiro-Garcia A; De Clercq E; Pannecouque C; Witvrouw M; Loftus T L; Turpin J A; Buckheit R W; Fanwick P E; Cushman M
Synthesis and anti-HIV activity of cosalane analogues incorporating two dichlorodisalicylmethane pharmacophore fragments.
Bioorganic & medicinal chemistry 2001;9(11):2827-41.
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2001: Zhang Y; de Bolle L; Aquaro S; van Lommel A; De Clercq E; Schols D
Productive infection of primary macrophages with human herpesvirus 7.
Journal of virology 2001;75(21):10511-4.
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2001: Gorry P R; Bristol G; Zack J A; Ritola K; Swanstrom R; Birch C J; Bell J E; Bannert N; Crawford K; Wang H; Schols D; De Clercq E; Kunstman K; Wolinsky S M; Gabuzda D
Macrophage tropism of human immunodeficiency virus type 1 isolates from brain and lymphoid tissues predicts neurotropism independent of coreceptor specificity.
Journal of virology 2001;75(21):10073-89.
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2001: De Clercq E
New developments in anti-HIV chemotherapy.
Current medicinal chemistry 2001;8(13):1543-72.
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2001: Moukha-Hafiq O; Taha M L; Lazrek H B; Vasseur J J; Pannecouque C; Witvrouw M; De Clercq E
Synthesis and biological evaluation of some 4-substituted 1-[1-(4-hydroxybutyl)-1,2,3-triazol-(4 &5)-ylmethyl]-1H-pyrazolo- 13,4-dipyrimidines.
Nucleosides, nucleotides & nucleic acids 2001;20(10-11):1811-21.
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2001: Moukha-Chafiq O; Taha M L; Lazrek H B; Pannecouque C; Witvrouw M; De Clercq E; Barascut J L; Imbach J L
Synthesis and biological activity of 4-substituted 1-[1-(2-hydroxyethoxy)-methyl-1,2,3-triazol-(4 & 5)-ylmethyl]-1H-pyrazolo[3,4-d]pyrimidines.
Nucleosides, nucleotides & nucleic acids 2001;20(10-11):1797-810.
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2001: De Clercq E
Hamao Umezawa Memorial Award Lecture: "An Odyssey in the Viral Chemotherapy Field".
International journal of antimicrobial agents 2001;18(4):309-28.
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2001: Snoeck R; Van Laethem Y; De Clercq E; De Maubeuge J; Clumeck N
Treatment of a bowenoid papulosis of the penis with local applications of cidofovir in a patient with acquired immunodeficiency syndrome.
Archives of internal medicine 2001;161(19):2382-4.
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2001: Hillenkamp J; Reinhard T; Ross R S; Böhringer D; Cartsburg O; Roggendorf M; De Clercq E; Godehardt E; Sundmacher R
Topical treatment of acute adenoviral keratoconjunctivitis with 0.2% cidofovir and 1% cyclosporine: a controlled clinical pilot study.
Archives of ophthalmology 2001;119(10):1487-91.
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2001: Matthys P; Hatse S; Vermeire K; Wuyts A; Bridger G; Henson G W; De Clercq E; Billiau A; Schols D
AMD3100, a potent and specific antagonist of the stromal cell-derived factor-1 chemokine receptor CXCR4, inhibits autoimmune joint inflammation in IFN-gamma receptor-deficient mice.
Journal of immunology (Baltimore, Md. : 1950) 2001;167(8):4686-92.
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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.
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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.
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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.
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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.
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2001: Snoeck R; Bossens M; Parent D; Delaere B; Degreef H; Van Ranst M; Noël J C; Wulfsohn M S; Rooney J F; Jaffe H S; De Clercq E
Phase II double-blind, placebo-controlled study of the safety and efficacy of cidofovir topical gel for the treatment of patients with human papillomavirus infection.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America 2001;33(5):597-602.
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2001: Pluymers W; De Clercq E; Debyser Z
HIV-1 integration as a target for antiretroviral therapy: a review.
Current drug targets. Infectious disorders 2001;1(2):133-49.
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2001: Rejman D; Masojídková M; De Clercq E; Rosenberg I
2'C-alkoxy and 2'-C-aryloxy derivatives of N-(2-phosphonomethoxyethyl)-purines and -pyrimidines: synthesis and biological activity.
Nucleosides, nucleotides & nucleic acids 2001;20(8):1497-522.
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2001: Redwane N; Lazrek H B; Barascut J L; Imbach J L; Balzarini J; Witvrouw M; De Clercq E
Synthesis and biological activities of (Z) and (E) alpha-ethenyl acyclonucleosides.
Nucleosides, nucleotides & nucleic acids 2001;20(8):1439-47.
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2001: Vlieghe P; Clerc T; Pannecouque C; Witvrouw M; De Clercq E; Salles J P; Kraus J L
New 3'-azido-3'-deoxythymidin-5'-yl O-(4-hydroxyalkyl or -alkenyl or -alkylepoxide) carbonate prodrugs: synthesis and anti-HIV evaluation.
Journal of medicinal chemistry 2001;44(18):3014-21.
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2001: Stamatiou G; Kolocouris A; Kolocouris N; Fytas G; Foscolos G B; Neyts J; De Clercq E
Novel 3-(2-adamantyl)pyrrolidines with potent activity against influenza A virus-identification of aminoadamantane derivatives bearing two pharmacophoric amine groups.
Bioorganic & medicinal chemistry letters 2001;11(16):2137-42.
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2001: Apers S; Baronikova S; Sindambiwe J B; Witvrouw M; De Clercq E; Vanden Berghe D; Van Marck E; Vlietinck A; Pieters L
Antiviral, haemolytic and molluscicidal activities of triterpenoid saponins from Maesa lanceolata: establishment of structure-activity relationships.
Planta medica 2001;67(6):528-32.
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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.
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2001: Geerinck K; Lukito G; Snoeck R; De Vos R; De Clercq E; Vanrenterghem Y; Degreef H; Maes B
A case of human orf in an immunocompromised patient treated successfully with cidofovir cream.
Journal of medical virology 2001;64(4):543-9.
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2001: Daelemans D; De Clercq E; Vandamme A M
A quantitative GFP-based bioassay for the detection of HIV-1 Tat transactivation inhibitors.
Journal of virological methods 2001;96(2):183-8.
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2001: De Clercq E
Antiviral drugs: current state of the art.
Journal of clinical virology : the official publication of the Pan American Society for Clinical Virology 2001;22(1):73-89.
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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.
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2001: Struyf S; Menten P; Lenaerts J P; Put W; D'Haese A; De Clercq E; Schols D; Proost P; Van Damme J
Diverging binding capacities of natural LD78beta isoforms of macrophage inflammatory protein-1alpha to the CC chemokine receptors 1, 3 and 5 affect their anti-HIV-1 activity and chemotactic potencies for neutrophils and eosinophils.
European journal of immunology 2001;31(7):2170-8.
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2001: Liekens S; Neyts J; De Clercq E; Verbeken E; Ribatti D; Presta M
Inhibition of fibroblast growth factor-2-induced vascular tumor formation by the acyclic nucleoside phosphonate cidofovir.
Cancer research 2001;61(13):5057-64.
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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.
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2001: Hatse S; Princen K; Gerlach L O; Bridger G; Henson G; De Clercq E; Schwartz T W; Schols D
Mutation of Asp(171) and Asp(262) of the chemokine receptor CXCR4 impairs its coreceptor function for human immunodeficiency virus-1 entry and abrogates the antagonistic activity of AMD3100.
Molecular pharmacology 2001;60(1):164-73.
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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.
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2001: Andrei G; Fiten P; De Clercq E; Snoeck R; Opdenakker G
Evaluating phenotype and genotype of drug-resistant strains in herpesviruses.
Molecular biotechnology 2001;18(2):155-67.
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2001: Herdewijn P; De Clercq E
The cyclohexene ring as bioisostere of a furanose ring: synthesis and antiviral activity of cyclohexenyl nucleosides.
Bioorganic & medicinal chemistry letters 2001;11(12):1591-7.
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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.
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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.
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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.
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2001: Vashishtha S C; Allen T M; Halleran S; Szydlowski J; Santos C L; De Clercq E; Balzarani J; Dimmock J R
Cytotoxic and anticancer properties of some 4-aryl-3-arylcarbonyl-1-ethyl-4-piperidinols and related compounds.
Die Pharmazie 2001;56(5):390-3.
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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.
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2001: Stephens C E; Felder T M; Sowell J W; Andrei G; Balzarini J; Snoeck R; De Clercq E
Synthesis and antiviral/antitumor evaluation of 2-amino- and 2-carboxamido-3-arylsulfonylthiophenes and related compounds as a new class of diarylsulfones.
Bioorganic & medicinal chemistry 2001;9(5):1123-32.
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2001: Mavromoustakos T; Calogeropoulou T; Koufaki M; Kolocouris A; Daliani I; Demetzos C; Meng Z; Makriyannis A; Balzarini J; De Clercq E
Ether phospholipid-AZT conjugates possessing anti-HIV and antitumor cell activity. Synthesis, conformational analysis, and study of their thermal effects on membrane bilayers.
Journal of medicinal chemistry 2001;44(11):1702-9.
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2001: Aquaro S; Menten P; Struyf S; Proost P; Van Damme J; De Clercq E; Schols D
The LD78beta isoform of MIP-1alpha is the most potent CC-chemokine in inhibiting CCR5-dependent human immunodeficiency virus type 1 replication in human macrophages.
Journal of virology 2001;75(9):4402-6.
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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.
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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.
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2001: Wang J; Froeyen M; Hendrix C; Andrei C; Snoeck R; Lescrinier E; De Clercq E; Herdewijn P
(D)- and (L)-cyclohexenyl-G, a new class of antiviral agents: synthesis, conformational analysis, molecular modeling, and biological activity.
Nucleosides, nucleotides & nucleic acids 2001;20(4-7):727-30.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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2001: De Clercq E
Vaccinia virus inhibitors as a paradigm for the chemotherapy of poxvirus infections.
Clinical microbiology reviews 2001;14(2):382-97.
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2001: Liekens S; Verbeken E; De Clercq E; Neyts J
Potent inhibition of hemangiosarcoma development in mice by cidofovir.
International journal of cancer. Journal international du cancer 2001;92(2):161-7.
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2001: De Clercq E
2001 ASPET Otto Krayer Award Lecture. Molecular targets for antiviral agents.
The Journal of pharmacology and experimental therapeutics 2001;297(1):1-10.
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2001: Naesens L; De Clercq E
Recent developments in herpesvirus therapy.
Herpes : the journal of the IHMF 2001;8(1):12-6.
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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.
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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.
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2001: Van Vaerenbergh K; Debaisieux L; De Cabooter N; Declercq C; Desmet K; Fransen K; Maes B; Marissens D; Miller K; Muyldermans G; Sprecher S; Stuyver L; Vaira D; Verhofstede C; Zissis G; Van Ranst M; De Clercq E; Desmyter J; Vandamme A M
Prevalence of genotypic resistance among antiretroviral drug-naive HIV-1-infected patients in Belgium.
Antiviral therapy 2001;6(1):63-70.
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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.
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2001: Balzarinia J; Degrève B; Zhu C; Durini E; Porcu L; De Clercq E; Karlsson A; Manfredini S
2'-O-Acyl/alkyl-substituted arabinosyl nucleosides as inhibitors of human mitochondrial thymidine kinase.
Biochemical pharmacology 2001;61(6):727-32.
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2001: Vlieghe P; Bihel F; Clerc T; Pannecouque C; Witvrouw M; De Clercq E; Salles J P; Chermann J C; Kraus J L
New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation.
Journal of medicinal chemistry 2001;44(5):777-86.
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2001: Santhosh K C; Paul G C; De Clercq E; Pannecouque C; Witvrouw M; Loftus T L; Turpin J A; Buckheit R W; Cushman M
Correlation of anti-HIV activity with anion spacing in a series of cosalane analogues with extended polycarboxylate pharmacophores.
Journal of medicinal chemistry 2001;44(5):703-14.
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2001: Varvaresou A; Iakovou K; Filippatos E; Souli C; Calogeropoulou T; Ioannidou I; Kourounakis A P; Pannecouque C; Witvrouw M; Padalko E; Neyts J; De Clercq E; Tsotinis A
Synthesis, antiretroviral and antioxidant evaluation of a series of new benzo[b]furan derivatives.
Arzneimittel-Forschung 2001;51(2):156-62.
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2001: Neyts J; De Clercq E
The anti-herpesvirus activity of (1'S,2'R)-9-[[1',2'-bis(hydroxymethyl)-cycloprop-1'-yl]methyl]guanine is markedly potentiated by the immunosuppressive agent mycophenolate mofetil.
Antiviral research 2001;49(2):121-7.
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2001: Neyts J; Naesens L; Ying C; De Bolle L; De Clercq E
Anti-herpesvirus activity of (1'S,2'R)-9-[[1',2'-bis(hydroxymethyl)-cycloprop-1'-yl]methyl] x guanine (A-5021) in vitro and in vivo.
Antiviral research 2001;49(2):115-20.
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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.
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2001: Liekens S; De Clercq E; Neyts J
Angiogenesis: regulators and clinical applications.
Biochemical pharmacology 2001;61(3):253-70.
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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.
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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.
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2001: Degrève B; Esnouf R; De Clercq E; Balzarini J
Mutation of Gln125 to Asn selectively abolishes the thymidylate kinase activity of herpes simplex virus type 1 thymidine kinase.
Molecular pharmacology 2001;59(2):285-93.
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2001: De Clercq E
New developments in anti-HIV chemotherapy.
Farmaco (Società chimica italiana : 1989) 2001;56(1-2):3-12.
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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.
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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.
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2001: Goebel F D; Hemmer R; Schmit J C; Bogner J R; de Clercq E; Witvrouw M; Pannecouque C; Valeyev R; Vandevelde M; Margery H; Tassignon J P
Phase I/II dose escalation and randomized withdrawal study with add-on azodicarbonamide in patients failing on current antiretroviral therapy.
AIDS (London, England) 2001;15(1):33-45.
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2001: Neyts J; De Clercq E
Efficacy of 2-amino-7-(1,3-dihydroxy-2-propoxymethyl)purine for treatment of vaccinia virus (orthopoxvirus) infections in mice.
Antimicrobial agents and chemotherapy 2001;45(1):84-7.
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2001: De Clercq E; Schols D
Inhibition of HIV infection by CXCR4 and CCR5 chemokine receptor antagonists.
Antiviral chemistry & chemotherapy 2001;12 Suppl 1():19-31.
-
2001: Snoeck R; Andrei G; De Clercq E
Cidofovir in the treatment of HPV-associated lesions.
Verhandelingen - Koninklijke Academie voor Geneeskunde van België 2001;63(2):93-120, discussion 120-2.
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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.
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2001: Debyser Z; Cherepanov P; Pluymers W; De Clercq E
Assays for the evaluation of HIV-1 integrase inhibitors.
Methods in molecular biology (Clifton, N.J.) 2001;160():139-55.
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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.
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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.
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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.
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2000: Van Gelder J; Deferme S; Annaert P; Naesens L; De Clercq E; Van den Mooter G; Kinget R; Augustijns P
Increased absorption of the antiviral ester prodrug tenofovir disoproxil in rat ileum by inhibiting its intestinal metabolism.
Drug metabolism and disposition: the biological fate of chemicals 2000;28(12):1394-6.
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2000: Degrève B; Esnouf R; De Clercq E; Balzarini J
Selective abolishment of pyrimidine nucleoside kinase activity of herpes simplex virus type 1 thymidine kinase by mutation of alanine-167 to tyrosine.
Molecular pharmacology 2000;58(6):1326-32.
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2000: Baekelandt V; Claeys A; Cherepanov P; De Clercq E; De Strooper B; Nuttin B; Debyser Z
DNA-Dependent protein kinase is not required for efficient lentivirus integration.
Journal of virology 2000;74(23):11278-85.
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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: Ying C; De Clercq E; Neyts J
Ribavirin and mycophenolic acid potentiate the activity of guanine- and diaminopurine-based nucleoside analogues against hepatitis B virus.
Antiviral research 2000;48(2):117-24.
-
2000: Santhosh K C; De Clercq E; Pannecouque C; Witvrouw M; Loftus T L; Turpin J A; Buckheit R W; Cushman M
Anti-HIV activity of a series of cosalane amino acid conjugates.
Bioorganic & medicinal chemistry letters 2000;10(22):2505-8.
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2000: Witvrouw M; Fikkert V; Pluymers W; Matthews B; Mardel K; Schols D; Raff J; Debyser Z; De Clercq E; Holan G; Pannecouque C
Polyanionic (i.e., polysulfonate) dendrimers can inhibit the replication of human immunodeficiency virus by interfering with both virus adsorption and later steps (reverse transcriptase/integrase) in the virus replicative cycle.
Molecular pharmacology 2000;58(5):1100-8.
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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: De Clercq E
Guanosine analogues as anti-herpesvirus agents.
Nucleosides, nucleotides & nucleic acids 2000;19(10-12):1531-41.
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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.
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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.
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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.
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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.
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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.
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2000: Degrève B; De Clercq E; Balzarini J
Selection of HSV-1 TK gene-transfected murine mammary carcinoma cells resistant to (E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU) and ganciclovir (GCV).
Gene therapy 2000;7(18):1543-52.
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2000: Van Gelder J; Shafiee M; De Clercq E; Penninckx F; Van den Mooter G; Kinget R; Augustijns P
Species-dependent and site-specific intestinal metabolism of ester prodrugs.
International journal of pharmaceutics 2000;205(1-2):93-100.
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2000: Paul G C; De Clercq E; Pannecouque C; Witvrouw M; Loftus T L; Turpin J A; Buckheit R W; Cushman M
Identification of optimal anion spacing for anti-HIV activity in a series of cosalane tetracarboxylates.
Bioorganic & medicinal chemistry letters 2000;10(18):2149-52.
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2000: Pluymers W; Neamati N; Pannecouque C; Fikkert V; Marchand C; Burke T R; Pommier Y; Schols D; De Clercq E; Debyser Z; Witvrouw M
Viral entry as the primary target for the anti-HIV activity of chicoric acid and its tetra-acetyl esters.
Molecular pharmacology 2000;58(3):641-8.
-
2000: De Clercq E
Current lead natural products for the chemotherapy of human immunodeficiency virus (HIV) infection.
Medicinal research reviews 2000;20(5):323-49.
-
2000: Snoeck R; Andrei G; De Clercq E
Novel agents for the therapy of varicella-zoster virus infections.
Expert opinion on investigational drugs 2000;9(8):1743-51.
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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.
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2000: Annaert P; Tukker J J; van Gelder J; Naesens L; de Clercq E; van Den Mooter G; Kinget R; Augustijns P
In vitro, ex vivo, and in situ intestinal absorption characteristics of the antiviral ester prodrug adefovir dipivoxil.
Journal of pharmaceutical sciences 2000;89(8):1054-62.
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2000: Van Vaerenbergh K; Van Laethem K; Albert J; Boucher C A; Clotet B; Floridia M; Gerstoft J; Hejdeman B; Nielsen C; Pannecouque C; Perrin L; Pirillo M F; Ruiz L; Schmit J C; Schneider F; Schoolmeester A; Schuurman R; Stellbrink H J; Stuyver L; Van Lunzen J; Van Remoortel B; Van Wijngaerden E; Vella S; Witvrouw M; Yerly S; De Clercq E; Destmyer J; Vandamme A M
Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues.
Antimicrobial agents and chemotherapy 2000;44(8):2109-17.
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2000: De Clercq E
Novel compounds in preclinical/early clinical development for the treatment of HIV infections.
Reviews in medical virology 2000;10(4):255-77.
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2000: Cherepanov P; Pluymers W; Claeys A; Proost P; De Clercq E; Debyser Z
High-level expression of active HIV-1 integrase from a synthetic gene in human cells.
The FASEB journal : official publication of the Federation of American Societies for Experimental Biology 2000;14(10):1389-99.
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2000: Al-Masoudi N A; Al-Soud Y A; Eherman M; De Clercq E
Synthesis of acyclic 6,7-dihaloquinolone nucleoside analogues as potential antibacterial and antiviral agents.
Bioorganic & medicinal chemistry 2000;8(6):1407-13.
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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.
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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.
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2000: Witvrouw M; Pannecouque C; Desmyter J; De Clercq E; Andries K
In vitro evaluation of the effect of temporary removal of HIV drug pressure.
Antiviral research 2000;46(3):215-21.
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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.
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2000: Estrada E; Uriarte E; Montero A; Teijeira M; Santana L; De Clercq E
A novel approach for the virtual screening and rational design of anticancer compounds.
Journal of medicinal chemistry 2000;43(10):1975-85.
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2000: Jonckheere H; De Clercq E; Anné J
Fidelity analysis of HIV-1 reverse transcriptase mutants with an altered amino-acid sequence at residues Leu74, Glu89, Tyr115, Tyr183 and Met184.
European journal of biochemistry / FEBS 2000;267(9):2658-65.
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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.
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2000: De Clercq E
Inhibition of HIV infection by bicyclams, highly potent and specific CXCR4 antagonists.
Molecular pharmacology 2000;57(5):833-9.
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2000: Neyts J; Kristmundsdóttir T; De Clercq E; Thormar H
Hydrogels containing monocaprin prevent intravaginal and intracutaneous infections with HSV-2 in mice: impact on the search for vaginal microbicides.
Journal of medical virology 2000;61(1):107-10.
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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.
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2000: Van Vaerenbergh K; Van Laethem K; Van Wijngaerden E; Schmit J C; Schneider F; Ruiz L; Clotet B; Verhofstede C; Van Wanzeele F; Muyldermans G; Simons P; Stuyver L; Hermans P; Evans C; De Clercq E; Desmyter J; Vandamme A M
Baseline HIV type 1 genotypic resistance to a newly added nucleoside analog is predictive of virologic failure of the new therapy.
AIDS research and human retroviruses 2000;16(6):529-37.
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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.
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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.
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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.
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2000: Andrei G; Snoeck R; Neyts J; Sandvold M L; Myhren F; De Clercq E
Antiviral activity of ganciclovir elaidic acid ester against herpesviruses.
Antiviral research 2000;45(3):157-67.
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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.
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2000: Ying C; De Clercq E; Nicholson W; Furman P; Neyts J
Inhibition of the replication of the DNA polymerase M550V mutation variant of human hepatitis B virus by adefovir, tenofovir, L-FMAU, DAPD, penciclovir and lobucavir.
Journal of viral hepatitis 2000;7(2):161-5.
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2000: Wnuk S F; Valdez C A; Khan J; Moutinho P; Robins M J; Yang X; Borchardt R T; Balzarini J; De Clercq E
Doubly homologated dihalovinyl and acetylene analogues of adenosine: synthesis, interaction with S-adenosyl-L-homocysteine hydrolase, and antiviral and cytostatic effects.
Journal of medicinal chemistry 2000;43(6):1180-6.
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2000: Jonckheere H; Anné J; De Clercq E
The HIV-1 reverse transcription (RT) process as target for RT inhibitors.
Medicinal research reviews 2000;20(2):129-54.
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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.
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2000: Witvrouw M; Weigold H; Pannecouque C; Schols D; De Clercq E; Holan G
Potent anti-HIV (type 1 and type 2) activity of polyoxometalates: structure-activity relationship and mechanism of action.
Journal of medicinal chemistry 2000;43(5):778-83.
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2000: Andrei G; Snoeck R; De Clercq E; Esnouf R; Fiten P; Opdenakker G
Resistance of herpes simplex virus type 1 against different phosphonylmethoxyalkyl derivatives of purines and pyrimidines due to specific mutations in the viral DNA polymerase gene.
The Journal of general virology 2000;81(Pt 3):639-48.
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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.
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2000: Teran C; Santana L; Teijeira M; Uriarte E; De Clercq E
Design, synthesis, conformational analysis and biological activities of purine-based 1,2-di-substituted carbocyclic nucleosides.
Chemical & pharmaceutical bulletin 2000;48(2):293-5.
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2000: Wang J; Froeyen M; Hendrix C; Andrei G; Snoeck R; De Clercq E; Herdewijn P
The cyclohexene ring system as a furanose mimic: synthesis and antiviral activity of both enantiomers of cyclohexenylguanine.
Journal of medicinal chemistry 2000;43(4):736-45.
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2000: Zhang Y; Hatse S; De Clercq E; Schols D
CXC-chemokine receptor 4 is not a coreceptor for human herpesvirus 7 entry into CD4(+) T cells.
Journal of virology 2000;74(4):2011-6.
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2000: Snoeck R; Noel J C; Muller C; De Clercq E; Bossens M
Cidofovir, a new approach for the treatment of cervix intraepithelial neoplasia grade III (CIN III).
Journal of medical virology 2000;60(2):205-9.
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2000: Casimiro-Garcia A; De Clercq E; Pannecouque C; Witvrouw M; Stup T L; Turpin J A; Buckheit R W; Cushman M
Synthesis and anti-HIV activity of cosalane analogues incorporating nitrogen in the linker chain.
Bioorganic & medicinal chemistry 2000;8(1):191-200.
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2000: Ying C; De Clercq E; Neyts J
Lamivudine, adefovir and tenofovir exhibit long-lasting anti-hepatitis B virus activity in cell culture.
Journal of viral hepatitis 2000;7(1):79-83.
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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.
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2000: Leyssen P; De Clercq E; Neyts J
Perspectives for the treatment of infections with Flaviviridae.
Clinical microbiology reviews 2000;13(1):67-82, table of contents.
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2000: Daelemans D; Schols D; Witvrouw M; Pannecouque C; Hatse S; van Dooren S; Hamy F; Klimkait T; de Clercq E; VanDamme A M
A second target for the peptoid Tat/transactivation response element inhibitor CGP64222: inhibition of human immunodeficiency virus replication by blocking CXC-chemokine receptor 4-mediated virus entry.
Molecular pharmacology 2000;57(1):116-24.
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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.
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2000: Blanco J; Barretina J; Henson G; Bridger G; De Clercq E; Clotet B; Esté J A
The CXCR4 antagonist AMD3100 efficiently inhibits cell-surface-expressed human immunodeficiency virus type 1 envelope-induced apoptosis.
Antimicrobial agents and chemotherapy 2000;44(1):51-6.
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2000: Schramm B; Penn M L; Speck R F; Chan S Y; De Clercq E; Schols D; Connor R I; Goldsmith M A
Viral entry through CXCR4 is a pathogenic factor and therapeutic target in human immunodeficiency virus type 1 disease.
Journal of virology 2000;74(1):184-92.
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2000: Andrei G; Snoeck R; Schols D; De Clercq E
Induction of apoptosis by cidofovir in human papillomavirus (HPV)-positive cells.
Oncology research 2000;12(9-10):397-408.
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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.
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1999: Kolocouris A; Tataridis D; Fytas G; Mavromoustakos T; Foscolos G B; Kolocouris N; De Clercq E
Synthesis of 2-(2-adamantyl)piperidines and structure anti-influenza virus A activity relationship study using a combination of NMR spectroscopy and molecular modeling.
Bioorganic & medicinal chemistry letters 1999;9(24):3465-70.
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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.
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1999: Neyts J; De Clercq E
Hydroxyurea potentiates the antiherpesvirus activities of purine and pyrimidine nucleoside and nucleoside phosphonate analogs.
Antimicrobial agents and chemotherapy 1999;43(12):2885-92.
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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.
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1999: De Clercq E
The emerging role of fusion inhibitors in HIV infection.
Drugs in R&D 1999;2(5):321-31.
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1999: Cabrera C; Witvrouw M; Gutiérrez A; Clotet B; Kuipers M E; Swart P J; Meijer D K; Desmyter J; De Clercq E; Esté J A
Resistance of the human immunodeficiency virus to the inhibitory action of negatively charged albumins on virus binding to CD4.
AIDS research and human retroviruses 1999;15(17):1535-43.
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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.
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1999: Van Laethem K; Van Vaerenbergh K; Schmit J C; Sprecher S; Hermans P; De Vroey V; Schuurman R; Harrer T; Witvrouw M; Van Wijngaerden E; Stuyver L; Van Ranst M; Desmyter J; De Clercq E; Vandamme A M
Phenotypic assays and sequencing are less sensitive than point mutation assays for detection of resistance in mixed HIV-1 genotypic populations.
Journal of acquired immune deficiency syndromes (1999) 1999;22(2):107-18.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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1999: Bridger G J; Skerlj R T; Padmanabhan S; Martellucci S A; Henson G W; Struyf S; Witvrouw M; Schols D; De Clercq E
Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-azamacrocycles that inhibit HIV-1 and HIV-2 replication by antagonism of the chemokine receptor CXCR4.
Journal of medicinal chemistry 1999;42(19):3971-81.
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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.
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1999: Van Gelder J; Witvrouw M; Pannecouque C; Henson G; Bridger G; Naesens L; De Clercq E; Annaert P; Shafiee M; Van den Mooter G; Kinget R; Augustijns P
Evaluation of the potential of ion pair formation to improve the oral absorption of two potent antiviral compounds, AMD3100 and PMPA.
International journal of pharmaceutics 1999;186(2):127-36.
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1999: Yi Y; Isaacs S N; Williams D A; Frank I; Schols D; De Clercq E; Kolson D L; Collman R G
Role of CXCR4 in cell-cell fusion and infection of monocyte-derived macrophages by primary human immunodeficiency virus type 1 (HIV-1) strains: two distinct mechanisms of HIV-1 dual tropism.
Journal of virology 1999;73(9):7117-25.
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1999: Ying C; Van Pelt J; Yap S H; De Clercq E; Neyts J
Use of digoxigenin-labelled probes for the quantitation of HBV-DNA in antiviral drug evaluation.
Journal of virological methods 1999;81(1-2):155-8.
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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.
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1999: Zhang Y; Schols D; De Clercq E
Selective activity of various antiviral compounds against HHV-7 infection.
Antiviral research 1999;43(1):23-35.
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1999: Witvrouw M; Pannecouque C; Van Laethem K; Desmyter J; De Clercq E; Vandamme A M
Activity of non-nucleoside reverse transcriptase inhibitors against HIV-2 and SIV.
AIDS (London, England) 1999;13(12):1477-83.
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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.
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1999: Menten P; Struyf S; Schutyser E; Wuyts A; De Clercq E; Schols D; Proost P; Van Damme J
The LD78beta isoform of MIP-1alpha is the most potent CCR5 agonist and HIV-1-inhibiting chemokine.
The Journal of clinical investigation 1999;104(4):R1-5.
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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.
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1999: Egberink H F; De Clercq E; Van Vliet A L; Balzarini J; Bridger G J; Henson G; Horzinek M C; Schols D
Bicyclams, selective antagonists of the human chemokine receptor CXCR4, potently inhibit feline immunodeficiency virus replication.
Journal of virology 1999;73(8):6346-52.
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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.
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1999: Van Gelder J; Annaert P; Naesens L; De Clercq E; Van den Mooter G; Kinget R; Augustijns P
Inhibition of intestinal metabolism of the antiviral ester prodrug bis(POC)-PMPA by nature-identical fruit extracts as a strategy to enhance its oral absorption: an in vitro study.
Pharmaceutical research 1999;16(7):1035-40.
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1999: Hibbitts S; Reeves J D; Simmons G; Gray P W; Epstein L G; Schols D; de Clercq E; Wells T N; Proudfoot A E; Clapham P R
Coreceptor ligand inhibition of fetal brain cell infection by HIV type 1.
AIDS research and human retroviruses 1999;15(11):989-1000.
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1999: De Bruyne T; Pieters L; Witvrouw M; De Clercq E; Vanden Berghe D; Vlietinck A J
Biological evaluation of proanthocyanidin dimers and related polyphenols.
Journal of natural products 1999;62(7):954-8.
-
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: De Clercq E
Perspectives for the treatment of hepatitis B virus infections.
International journal of antimicrobial agents 1999;12(2):81-95.
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1999: Raic-Malic S; Hergold-Brundic A; Nagl A; Grdisa M; Pavelic K; De Clercq E; Mintas M
Novel pyrimidine and purine derivatives of L-ascorbic acid: synthesis and biological evaluation.
Journal of medicinal chemistry 1999;42(14):2673-8.
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1999: Liekens S; Leali D; Neyts J; Esnouf R; Rusnati M; Dell'Era P; Maudgal P C; De Clercq E; Presta M
Modulation of fibroblast growth factor-2 receptor binding, signaling, and mitogenic activity by heparin-mimicking polysulfonated compounds.
Molecular pharmacology 1999;56(1):204-13.
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1999: Esté J A; Cabrera C; Blanco J; Gutierrez A; Bridger G; Henson G; Clotet B; Schols D; De Clercq E
Shift of clinical human immunodeficiency virus type 1 isolates from X4 to R5 and prevention of emergence of the syncytium-inducing phenotype by blockade of CXCR4.
Journal of virology 1999;73(7):5577-85.
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1999: Thormar H; Bergsson G; Gunnarsson E; Georgsson G; Witvrouw M; Steingrímsson O; De Clercq E; Kristmundsdóttir T
Hydrogels containing monocaprin have potent microbicidal activities against sexually transmitted viruses and bacteria in vitro.
Sexually transmitted infections 1999;75(3):181-5.
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1999: Smeijsters L J; Franssen F F; Naesens L; de Vries E; Holý A; Balzarini J; de Clercq E; Overdulve J P
Inhibition of the in vitro growth of Plasmodium falciparum by acyclic nucleoside phosphonates.
International journal of antimicrobial agents 1999;12(1):53-61.
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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.
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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.
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1999: Pluymers W; Cherepanov P; Schols D; De Clercq E; Debyser Z
Nuclear localization of human immunodeficiency virus type 1 integrase expressed as a fusion protein with green fluorescent protein.
Virology 1999;258(2):327-32.
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1999: Simonart T; Andrei G; Parent D; Van Vooren J P; De Clercq E; Snoeck R
In vitro sensitivity of Kaposi's sarcoma cells to various chemotherapeutic agents including acyclic nucleoside phosphonates.
Antiviral chemistry & chemotherapy 1999;10(3):129-34.
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1999: Blanco J; Jacotot E; Cabrera C; Cardona A; Clotet B; De Clercq E; Esté J A
The implication of the chemokine receptor CXCR4 in HIV-1 envelope protein-induced apoptosis is independent of the G protein-mediated signalling.
AIDS (London, England) 1999;13(8):909-17.
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1999: Witvrouw M; Pannecouque C; De Clercq E; Fernández-Alvarez E; Marco J L
Inhibition of human immunodeficiency virus type (HIV-1) replication by some diversely functionalized spirocyclopropyl derivatives.
Archiv der Pharmazie 1999;332(5):163-6.
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1999: Vandamme A M; Van Laethem K; Schmit J C; Van Wijngaerden E; Reynders M; Debyser Z; Witvrouw M; Van Ranst M; De Clercq E; Desmyter J
Long-term stability of human immunodeficiency virus viral load and infectivity in whole blood.
European journal of clinical investigation 1999;29(5):445-52.
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1999: Liekens S; Verbeken E; Vandeputte M; De Clercq E; Neyts J
A novel animal model for hemangiomas: inhibition of hemangioma development by the angiogenesis inhibitor TNP-470.
Cancer research 1999;59(10):2376-83.
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1999: Cherepanov P; Surratt D; Toelen J; Pluymers W; Griffith J; De Clercq E; Debyser Z
Activity of recombinant HIV-1 integrase on mini-HIV DNA.
Nucleic acids research 1999;27(10):2202-10.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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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.
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1999: Struyf S; Proost P; Schols D; De Clercq E; Opdenakker G; Lenaerts J P; Detheux M; Parmentier M; De Meester I; Scharpé S; Van Damme J
CD26/dipeptidyl-peptidase IV down-regulates the eosinophil chemotactic potency, but not the anti-HIV activity of human eotaxin by affecting its interaction with CC chemokine receptor 3.
Journal of immunology (Baltimore, Md. : 1950) 1999;162(8):4903-9.
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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.
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1999: Niyonzima G; Laekeman G; Witvrouw M; Van Poel B; Pieters L; Paper D; De Clercq E; Franz G; Vlietinck A J
Hypoglycemic, anticomplement and anti-HIV activities of Spathodea campanulata stem bark.
Phytomedicine : international journal of phytotherapy and phytopharmacology 1999;6(1):45-9.
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1999: Vandamme A M; Van Laethem K; De Clercq E
Managing resistance to anti-HIV drugs: an important consideration for effective disease management.
Drugs 1999;57(3):337-61.
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1999: Neyts J; De Clercq E
The immunosuppressive agent mycophenolate mofetil markedly potentiates the activity of lobucavir [1R(1alpha,2beta,3alpha)]-9-[2,3-bis(hydroxymethyl)cyclobutyl]guanine against different herpes viruses.
Transplantation 1999;67(5):760-4.
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1999: Degrève B; De Clercq E; Balzarini J
Bystander effect of purine nucleoside analogues in HSV-1 tk suicide gene therapy is superior to that of pyrimidine nucleoside analogues.
Gene therapy 1999;6(2):162-70.
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1999: Snoeck R; Andrei G; De Clercq E
Current pharmacological approaches to the therapy of varicella zoster virus infections: a guide to treatment.
Drugs 1999;57(2):187-206.
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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.
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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.
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1999: De Clercq E
Perspectives of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection.
Farmaco (Società chimica italiana : 1989) 1999;54(1-2):26-45.
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1999: Daelemans D; Vandamme A M; De Clercq E
Human immunodeficiency virus gene regulation as a target for antiviral chemotherapy.
Antiviral chemistry & chemotherapy 1999;10(1):1-14.
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1999: Esté J A; Cabrera C; De Clercq E; Struyf S; Van Damme J; Bridger G; Skerlj R T; Abrams M J; Henson G; Gutierrez A; Clotet B; Schols D
Activity of different bicyclam derivatives against human immunodeficiency virus depends on their interaction with the CXCR4 chemokine receptor.
Molecular pharmacology 1999;55(1):67-73.
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1999: Neyts J; Leyssen P; De Clercq E
Infections with flaviviridae.
Verhandelingen - Koninklijke Academie voor Geneeskunde van België 1999;61(6):661-97; discussion 697-9.
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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.
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1998: Snoeck R; Andrei G; De Clercq E
Specific therapies for human papilloma virus infections.
Current opinion in infectious diseases 1998;11(6):733-7.
-
1998: Neyts J; De Clercq E
Mycophenolate mofetil strongly potentiates the anti-herpesvirus activity of acyclovir.
Antiviral research 1998;40(1-2):53-6.
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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.
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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.
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1998: Neyts J; Andrei G; De Clercq E
The antiherpesvirus activity of H2G [(R)-9-[4-hydroxy-2-(hydroxymethyl)butyl]guanine] is markedly enhanced by the novel immunosuppressive agent mycophenolate mofetil.
Antimicrobial agents and chemotherapy 1998;42(12):3285-9.
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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.
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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.
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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.
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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.
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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.
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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; Naesens L; De Clercq E
New antivirals - mechanism of action and resistance development.
Current opinion in microbiology 1998;1(5):535-46.
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1998: Schols D; Proost P; Struyf S; Wuyts A; De Meester I; Scharpé S; Van Damme J; De Clercq E
CD26-processed RANTES(3-68), but not intact RANTES, has potent anti-HIV-1 activity.
Antiviral research 1998;39(3):175-87.
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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.
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1998: Schmit J C; Van Laethem K; Ruiz L; Hermans P; Sprecher S; Sönnerborg A; Leal M; Harrer T; Clotet B; Arendt V; Lissen E; Witvrouw M; Desmyter J; De Clercq E; Vandamme A M
Multiple dideoxynucleoside analogue-resistant (MddNR) HIV-1 strains isolated from patients from different European countries.
AIDS (London, England) 1998;12(15):2007-15.
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1998: Ostrowski T; Wroblowski B; Busson R; Rozenski J; De Clercq E; Bennett M S; Champness J N; Summers W C; Sanderson M R; Herdewijn P
5-Substituted pyrimidines with a 1,5-anhydro-2, 3-dideoxy-D-arabino-hexitol moiety at N-1: synthesis, antiviral activity, conformational analysis, and interaction with viral thymidine kinase.
Journal of medicinal chemistry 1998;41(22):4343-53.
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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.
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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.
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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.
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1998: Simmons G; Reeves J D; McKnight A; Dejucq N; Hibbitts S; Power C A; Aarons E; Schols D; De Clercq E; Proudfoot A E; Clapham P R
CXCR4 as a functional coreceptor for human immunodeficiency virus type 1 infection of primary macrophages.
Journal of virology 1998;72(10):8453-7.
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1998: Chimirri A; Grasso S; Monforte A M; Monforte P; Rao A; Zappalà M; Bruno G; Nicolò F; Pannecouque C; Witvrouw M; De Clercq E
Synthesis, structure and in vitro anti-human immunodeficiency virus activity of novel 3-methyl-1H,3H-thiazolo[3,4-a]benzimidazoles.
Antiviral chemistry & chemotherapy 1998;9(5):431-8.
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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.
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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.
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1998: Proost P; Struyf S; Wuyts A; Menten P; De Meester I; Lambeir A M; Scharpé S; Schols D; De Clercq E; Van Damme J
Isolation and identification of naturally modified C-C chemokines MCP-1, MCP-2 and RANTES: effects of posttranslational modifications on receptor usage, chemotactic and anti-HIV-1 activity.
European cytokine network 1998;9(3 Suppl):73-5.
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1998: Terán C; Santana L; Teijeira M; Uriarte E; Balzarini J; De Clercq E
Synthesis and chemotherapeutic activity of a carbocyclic analogue of tegafur.
Die Pharmazie 1998;53(9):644.
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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.
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1998: Schols D; De Clercq E
The simian immunodeficiency virus mnd(GB-1) strain uses CXCR4, not CCR5, as coreceptor for entry in human cells.
The Journal of general virology 1998;79 ( Pt 9)():2203-5.
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1998: Struyf S; Proost P; Sozzani S; Mantovani A; Wuyts A; De Clercq E; Schols D; Van Damme J
Enhanced anti-HIV-1 activity and altered chemotactic potency of NH2-terminally processed macrophage-derived chemokine (MDC) imply an additional MDC receptor.
Journal of immunology (Baltimore, Md. : 1950) 1998;161(6):2672-5.
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1998: Annaert P; Van Gelder J; Naesens L; De Clercq E; Van den Mooter G; Kinget R; Augustijns P
Carrier mechanisms involved in the transepithelial transport of bis(POM)-PMEA and its metabolites across Caco-2 monolayers.
Pharmaceutical research 1998;15(8):1168-73.
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1998: Suruga Y; Makino M; Okada Y; Tanaka H; De Clercq E; Baba M
Prevention of murine AIDS development by (R)-9-(2-phosphonylmethoxypropyl)adenine.
Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association 1998;18(4):316-22.
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1998: Proost P; Struyf S; Schols D; Durinx C; Wuyts A; Lenaerts J P; De Clercq E; De Meester I; Van Damme J
Processing by CD26/dipeptidyl-peptidase IV reduces the chemotactic and anti-HIV-1 activity of stromal-cell-derived factor-1alpha.
FEBS letters 1998;432(1-2):73-6.
-
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.
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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.
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1998: Schmit J C; Ruiz L; Stuyver L; Van Laethem K; Vanderlinden I; Puig T; Rossau R; Desmyter J; De Clercq E; Clotet B; Vandamme A M
Comparison of the LiPA HIV-1 RT test, selective PCR and direct solid phase sequencing for the detection of HIV-1 drug resistance mutations.
Journal of virological methods 1998;73(1):77-82.
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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.
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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.
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1998: Naesens L; Bischofberger N; Augustijns P; Annaert P; Van den Mooter G; Arimilli M N; Kim C U; De Clercq E
Antiretroviral efficacy and pharmacokinetics of oral bis(isopropyloxycarbonyloxymethyl)-9-(2-phosphonylmethoxypropyl)adenine in mice.
Antimicrobial agents and chemotherapy 1998;42(7):1568-73.
-
1998: Simonart T; Noel J C; De Dobbeleer G; Parent D; Van Vooren J P; De Clercq E; Snoeck R
Treatment of classical Kaposi's sarcoma with intralesional injections of cidofovir: report of a case.
Journal of medical virology 1998;55(3):215-8.
-
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: De Clercq E
The role of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection.
Antiviral research 1998;38(3):153-79.
-
1998: Seley K L; Schneller S W; De Clercq E; Rattendi D; Lane S; Bacchi C J; Korba B
The importance of the 4'-hydroxyl hydrogen for the anti-trypanosomal and antiviral properties of (+)-5'-noraristeromycin and two 7-deaza analogues.
Bioorganic & medicinal chemistry 1998;6(6):797-801.
-
1998: Liekens S; Andrei G; Vandeputte M; De Clercq E; Neyts J
Potent inhibition of hemangioma formation in rats by the acyclic nucleoside phosphonate analogue cidofovir.
Cancer research 1998;58(12):2562-7.
-
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.
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1998: Meerbach A; Holý A; Wutzler P; De Clercq E; Neyts J
Inhibitory effects of novel nucleoside and nucleotide analogues on Epstein-Barr virus replication.
Antiviral chemistry & chemotherapy 1998;9(3):275-82.
-
1998: Thormar H; Georgsson G; Gunnarsson E; Naesens L; Torsteinsdóttir S; Balzarini J; De Clercq E
Treatment of visna virus infection in lambs with the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)adenine (PMEA).
Antiviral chemistry & chemotherapy 1998;9(3):245-52.
-
1998: Vandamme A M; Van Vaerenbergh K; De Clercq E
Anti-human immunodeficiency virus drug combination strategies.
Antiviral chemistry & chemotherapy 1998;9(3):187-203.
-
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.
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1998: Schols D; Esté J A; Cabrera C; De Clercq E
T-cell-line-tropic human immunodeficiency virus type 1 that is made resistant to stromal cell-derived factor 1alpha contains mutations in the envelope gp120 but does not show a switch in coreceptor use.
Journal of virology 1998;72(5):4032-7.
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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.
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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.
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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.
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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.
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1998: Debyser Z; Van Wijngaerden E; Van Laethem K; Beuselinck K; Reynders M; De Clercq E; Desmyter J; Vandamme A M
Failure to quantify viral load with two of the three commercial methods in a pregnant woman harboring an HIV type 1 subtype G strain.
AIDS research and human retroviruses 1998;14(5):453-9.
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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.
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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.
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1998: Proost P; De Meester I; Schols D; Struyf S; Lambeir A M; Wuyts A; Opdenakker G; De Clercq E; Scharpé S; Van Damme J
Amino-terminal truncation of chemokines by CD26/dipeptidyl-peptidase IV. Conversion of RANTES into a potent inhibitor of monocyte chemotaxis and HIV-1-infection.
The Journal of biological chemistry 1998;273(13):7222-7.
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1998: Snoeck R; Wellens W; Desloovere C; Van Ranst M; Naesens L; De Clercq E; Feenstra L
Treatment of severe laryngeal papillomatosis with intralesional injections of cidofovir [(S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine].
Journal of medical virology 1998;54(3):219-25.
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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.
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1998: Van Laethem K; Beuselinck K; Van Dooren S; De Clercq E; Desmyter J; Vandamme A M
Diagnosis of human immunodeficiency virus infection by a polymerase chain reaction assay evaluated in patients harbouring strains of diverse geographical origin.
Journal of virological methods 1998;70(2):153-66.
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1998: Neyts J; Andrei G; De Clercq E
The novel immunosuppressive agent mycophenolate mofetil markedly potentiates the antiherpesvirus activities of acyclovir, ganciclovir, and penciclovir in vitro and in vivo.
Antimicrobial agents and chemotherapy 1998;42(2):216-22.
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1998: Annaert P; Gosselin G; Pompon A; Benzaria S; Valette G; Imbach J L; Naesens L; Hatse S; de Clercq E; Van den Mooter G; Kinget R; Augustijns P
Comparison of the disposition of ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA] in Caco-2 monolayers.
Pharmaceutical research 1998;15(2):239-45.
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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.
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1998: Jonckheere H; Witvrouw M; De Clercq E; Anné J
Lamivudine resistance of HIV type 1 does not delay development of resistance to nonnucleoside HIV type 1-specific reverse transcriptase inhibitors as compared with wild-type HIV type 1.
AIDS research and human retroviruses 1998;14(3):249-53.
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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.
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1998: Revankar G R; Ojwang J O; Mustain S D; Rando R F; De Clercq E; Huffman J H; Drach J C; Sommadossi J P; Lewis A F
Thiazolo[4,5-d]pyrimidines. Part II. Synthesis and anti-human cytomegalovirus activity in vitro of certain acyclonucleosides and acyclonucleotides derived from the guanine analogue 5-aminothiazolo[4,5-d]pyrimidine-2,7(3H,6H)-dione.
Antiviral chemistry & chemotherapy 1998;9(1):53-63.
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1998: De Clercq E
Carbocyclic adenosine analogues as S-adenosylhomocysteine hydrolase inhibitors and antiviral agents: recent advances.
Nucleosides & nucleotides 1998;17(1-3):625-34.
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1998: Daelemans D; Vandamme A M; Shuto S; Matsuda A; De Clercq E
Stereospecificity of 6'-C-neplanocin A analogues as inhibitors of S-adenosylhomocysteine hydrolase activity and human immunodeficiency virus replication.
Nucleosides & nucleotides 1998;17(1-3):479-86.
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1998: Efimtseva E V; Mikhailov S N; Fomicheva M V; Meshkov S V; Rodionov M S; Khomutov A R; De Clercq E
[Acyclic nucleotide analogues based on phosphonic acids]
Bioorganicheskaia khimiia 1998;24(1):16-20.
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1998: Papakonstantinou-Garoufalia S S; Tani E; Todoulou O; Papadaki-Valiraki A; Filippatos E; De Clercq E; Kourounakis P N
Synthesis and pharmacochemical investigation of some novel 1,2,4-4H-triazoles with potential antiviral activity.
The Journal of pharmacy and pharmacology 1998;50(1):117-24.
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1998: Neyts J; De Clercq E
In vitro and in vivo inhibition of murine gamma herpesvirus 68 replication by selected antiviral agents.
Antimicrobial agents and chemotherapy 1998;42(1):170-2.
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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.
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1998: Donzella G A; Schols D; Lin S W; Esté J A; Nagashima K A; Maddon P J; Allaway G P; Sakmar T P; Henson G; De Clercq E; Moore J P
AMD3100, a small molecule inhibitor of HIV-1 entry via the CXCR4 co-receptor.
Nature medicine 1998;4(1):72-7.
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1998: Andrei G; Snoeck R; Piette J; Delvenne P; De Clercq E
Inhibiting effects of cidofovir (HPMPC) on the growth of the human cervical carcinoma (SiHa) xenografts in athymic nude mice.
Oncology research 1998;10(10):533-9.
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1998: Andrei G; Snoeck R; Piette J; Delvenne P; De Clercq E
Antiproliferative effects of acyclic nucleoside phosphonates on human papillomavirus (HPV)-harboring cell lines compared with HPV-negative cell lines.
Oncology research 1998;10(10):523-31.
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1998: De Clercq E
New perspectives for the treatment of HIV infections.
Verhandelingen - Koninklijke Academie voor Geneeskunde van België 1998;60(1):13-41; discussion 41-5.
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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.
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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.
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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.
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1997: Neyts J; De Clercq E
Antiviral drug susceptibility of human herpesvirus 8.
Antimicrobial agents and chemotherapy 1997;41(12):2754-6.
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1997: De Vreese K; Van Nerum I; Vermeire K; Anné J; De Clercq E
Sensitivity of human immunodeficiency virus to bicyclam derivatives is influenced by the three-dimensional structure of gp120.
Antimicrobial agents and chemotherapy 1997;41(12):2616-20.
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1997: Daelemans D; Esté J A; Witvrouw M; Pannecouque C; Jonckheere H; Aquaro S; Perno C F; De Clercq E; Vandamme A M
S-adenosylhomocysteine hydrolase inhibitors interfere with the r