New developments in anti-HIV chemotherapy.
|
De Clercq E
|
|
Farmaco (Società chimica italiana : 1989)
|
Novel compounds in preclinical/early clinical development for the treatment of HIV infections.
|
De Clercq E
|
|
Reviews in medical virology
|
N-3 substituted TSAO derivatives as a probe to explore the dimeric interface of HIV-1 reverse transcriptase.
|
De Clercq E
|
|
Nucleosides, nucleotides & nucleic acids
|
Perspectives for the chemotherapy of AIDS.
|
De Clercq E
|
|
Anticancer research
|
[Current acquisitions in antiviral drugs (anti-HIV)].
|
De Clercq E
|
|
Journal de pharmacie de Belgique
|
Discovery, development and characterization of agents active against the AIDS virus.
|
De Clercq E
|
|
Journal of receptor and signal transduction research
|
Perspectives of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection.
|
De Clercq E
|
|
Farmaco (Società chimica italiana : 1989)
|
Enhanced inhibition of HIV-1 replication in macrophages by antisense oligonucleotides, ribozymes and acyclic nucleoside phosphonate analogs delivered in pH-sensitive liposomes.
|
De Clercq E
|
|
Nucleosides, nucleotides & nucleic acids
|
Discovery of Piperidine-Linked Pyridine Analogues as Potent Non-nucleoside HIV-1 Reverse Transcriptase Inhibitors.
|
De Clercq E
|
2013
|
ChemMedChem
|
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
|
De Clercq E
|
2013
|
Bioorganic & medicinal chemistry
|
Design, Synthesis, and Biological Evaluation of Novel 3,5-Disubstituted-1,2,6-Thiadiazine-1,1-Dione Derivatives as HIV-1 NNRTIs.
|
De Clercq E
|
2013
|
Chemical biology & drug design
|
Towards new C6-rigid S-DABO HIV-1 reverse transcriptase inhibitors: Synthesis, biological investigation and molecular modeling studies.
|
De Clercq E
|
2013
|
Bioorganic & medicinal chemistry
|
Novel piperidinylamino-diarylpyrimidine derivatives with dual structural conformations as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
2013
|
Bioorganic & medicinal chemistry letters
|
The Nucleoside Reverse Transcriptase Inhibitors, Nonnucleoside Reverse Transcriptase Inhibitors, and Protease Inhibitors in the Treatment of HIV Infections (AIDS).
|
De Clercq E
|
2013
|
Advances in pharmacology (San Diego, Calif.)
|
Molecular design, synthesis and biological evaluation of BP-O-DAPY and O-DAPY derivatives as non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
De Clercq E
|
2013
|
European journal of medicinal chemistry
|
Dancing with chemical formulae of antivirals: a personal account.
|
De Clercq E
|
2013
|
Biochemical pharmacology
|
Chiral resolution, absolute configuration assignment and biological activity of racemic diarylpyrimidine CH(OH)-DAPY as potent nonnucleoside HIV-1 reverse transcriptase inhibitors.
|
De Clercq E
|
2012
|
European journal of medicinal chemistry
|
The HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors (Part V ☆ ): Capravirine and Its Analogues.
|
De Clercq E
|
2012
|
Current medicinal chemistry
|
Recent progress in small molecule CCR5 antagonists as potential HIV-1 entry inhibitors.
|
De Clercq E
|
2012
|
Current pharmaceutical design
|
Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
|
De Clercq E
|
2012
|
Journal of medicinal chemistry
|
Dihydro-alkoxyl-benzyl-oxopyrimidine derivatives (DABOs) as non-nucleoside reverse transcriptase inhibitors: an update review (2001-2011).
|
De Clercq E
|
2012
|
Current medicinal chemistry
|
Recent advances in the research of 2,3-diaryl-1,3-thiazolidin-4-one derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
2012
|
Current medicinal chemistry
|
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
2012
|
Bioorganic & medicinal chemistry
|
Arylazolylthioacetanilide. Part 11: Design, Synthesis and Biological Evaluation of 1,2,4-Triazole Thioacetanilide Derivatives as Novel Non-Nucleoside HIV-1 Reverse Transcriptase Inhibitors.
|
De Clercq E
|
2012
|
Medicinal chemistry (Shāriqah (United Arab Emirates))
|
Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
2012
|
European journal of medicinal chemistry
|
Structure-based bioisosterism design, synthesis and biological evaluation of novel 1,2,4-triazin-6-ylthioacetamides as potent HIV-1 NNRTIs.
|
De Clercq E
|
2012
|
Bioorganic & medicinal chemistry letters
|
A 40-year journey in search of selective antiviral chemotherapy.
|
De Clercq E
|
2011
|
Annual review of pharmacology and toxicology
|
Recent advances in DAPYs and related analogues as HIV-1 NNRTIs.
|
De Clercq E
|
2011
|
Current medicinal chemistry
|
Synthesis and biological evaluation of 6-substituted 5-alkyl-2-(phenylaminocarbonylmethylthio)pyrimidin-4(3H)-ones as potent HIV-1 NNRTIs.
|
De Clercq E
|
2011
|
ChemMedChem
|
HIV-1 NNRTIs: Structural diversity, pharmacophore similarity, and implications for drug design.
|
De Clercq E
|
2011
|
Medicinal research reviews
|
Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
De Clercq E
|
2011
|
Bioorganic & medicinal chemistry
|
Synthesis and anti-HIV activity of aryl-2-[(4-cyanophenyl)amino]-4-pyrimidinone hydrazones as potent non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
2011
|
ChemMedChem
|
1,2,3-thiadiazole thioacetanilides. Part 2: Synthesis and biological evaluation of a new series of 2-{[4-(3,4-dichlorophenyl)-1,2,3-thiadiazol-5-yl]sulfanyl}acetanilides as HIV-1 inhibitors.
|
De Clercq E
|
2010
|
Chemistry & biodiversity
|
Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
De Clercq E
|
2010
|
Bioorganic & medicinal chemistry
|
Antiretroviral drugs.
|
De Clercq E
|
2010
|
Current opinion in pharmacology
|
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy.
|
De Clercq E
|
2010
|
Bioorganic & medicinal chemistry
|
Lead optimization of diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
|
De Clercq E
|
2010
|
ChemMedChem
|
Early nucleoside reverse transcriptase inhibitors for the treatment of HIV: a brief history of stavudine (D4T) and its comparison with other dideoxynucleosides.
|
De Clercq E
|
2010
|
Antiviral research
|
In search of a selective therapy of viral infections.
|
De Clercq E
|
2010
|
Antiviral research
|
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
|
De Clercq E
|
2010
|
Bioorganic & medicinal chemistry
|
Design strategies of novel NNRTIs to overcome drug resistance.
|
De Clercq E
|
2009
|
Current medicinal chemistry
|
Sulfanyltriazole/tetrazoles: a promising class of HIV-1 NNRTIs.
|
De Clercq E
|
2009
|
Mini reviews in medicinal chemistry
|
Crystallographic study of a novel subnanomolar inhibitor provides insight on the binding interactions of alkenyldiarylmethanes with human immunodeficiency virus-1 reverse transcriptase.
|
De Clercq E
|
2009
|
J Med Chem
|
Synthesis and studies of new 2-(coumarin-4-yloxy)-4,6-(substituted)-S-triazine derivatives as potential anti-HIV agents.
|
De Clercq E
|
2009
|
Archiv der Pharmazie
|
Drug targets in cytomegalovirus infection.
|
De Clercq E
|
2009
|
Infectious disorders drug targets
|
Anti-HIV drugs: 25 compounds approved within 25 years after the discovery of HIV.
|
De Clercq E
|
2009
|
International journal of antimicrobial agents
|
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.
|
De Clercq E
|
2009
|
European journal of medicinal chemistry
|
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.
|
De Clercq E
|
2009
|
European journal of medicinal chemistry
|
Design, synthesis, and SAR of naphthyl-substituted Diarylpyrimidines as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
|
De Clercq E
|
2009
|
ChemMedChem
|
Non-nucleoside reverse transcriptase inhibitors (Part 18): synthesis and anti-HIV activity of 4-allylamino or 4-azido substituted diaryltriazines.
|
De Clercq E
|
2009
|
Yao xue xue bao = Acta pharmaceutica Sinica
|
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.
|
De Clercq E
|
2009
|
Chemistry & biodiversity
|
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.
|
De Clercq E
|
2009
|
European journal of medicinal chemistry
|
1,2,3-Selenadiazole thioacetanilides: synthesis and anti-HIV activity evaluation.
|
De Clercq E
|
2009
|
Bioorganic & medicinal chemistry
|
A new drug combination therapy for treatment-naive patients with HIV-1 infection, consisting of raltegravir, emtricitabine and tenofovir disoproxil fumarate.
|
De Clercq E
|
2009
|
Expert opinion on pharmacotherapy
|
Emerging antiviral drugs.
|
De Clercq E
|
2008
|
Expert opinion on emerging drugs
|
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
2008
|
Bioorganic & medicinal chemistry
|
Mechanism of antiviral drug resistance of vaccinia virus: identification of residues in the viral DNA polymerase conferring differential resistance to antipoxvirus drugs.
|
De Clercq E
|
2008
|
J Virol
|
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.
|
De Clercq E
|
2008
|
Bioorganic & medicinal chemistry
|
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.
|
De Clercq E
|
2008
|
Chemistry & biodiversity
|
Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: structural modulations of diaryltriazines with potent anti-HIV activity.
|
De Clercq E
|
2008
|
European journal of medicinal chemistry
|
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).
|
De Clercq E
|
2008
|
Bioorganic & medicinal chemistry
|
Inhibition of tubulin polymerization by select alkenyldiarylmethanes.
|
De Clercq E
|
2008
|
Bioorganic & medicinal chemistry letters
|
Inhibition of human immunodeficiency virus type 1 replication in human cells by Debio-025, a novel cyclophilin binding agent.
|
De Clercq E
|
2008
|
Antimicrobial agents and chemotherapy
|
Investigation of the alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors as potential cAMP phosphodiesterase-4B2 inhibitors.
|
De Clercq E
|
2008
|
Bioorganic & medicinal chemistry letters
|
Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
|
De Clercq E
|
2008
|
European journal of medicinal chemistry
|
2-(2,6-Dihalo-phenyl)-3-heteroaryl-2-ylmethyl-1, 3-thiazolidin-4-ones: anti-HIV agents.
|
De Clercq E
|
2008
|
Chemical biology & drug design
|
1,2,3-Thiadiazole thioacetanilides as a novel class of potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
2008
|
Bioorganic & medicinal chemistry letters
|
Recent advances in the research of HIV-1 RNase H inhibitors.
|
De Clercq E
|
2008
|
Mini reviews in medicinal chemistry
|
Synthesis and evaluation of 2-(2,6-dihalophenyl)-3-pyrimidinyl-1,3-thiazolidin-4-one analogues as anti-HIV-1 agents.
|
De Clercq E
|
2007
|
Bioorganic & medicinal chemistry
|
Antiviral activity of 3-(3,5-dimethylbenzyl)uracil derivatives against HIV-1 and HCMV.
|
De Clercq E
|
2007
|
Nucleosides, nucleotides & nucleic acids
|
Nitroimidazoles Part 6. Synthesis, structure and in vitro anti-HIV activity of new 5-substituted piperazinyl-4-nitroimidazole derivatives.
|
De Clercq E
|
2007
|
Antiviral chemistry & chemotherapy
|
Synthesis and biological evaluation of 2,3-diaryl substituted-1,3-thiazolidin-4-ones as anti-HIV agents.
|
De Clercq E
|
2007
|
Medicinal chemistry (Shāriqah (United Arab Emirates))
|
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.
|
De Clercq E
|
2007
|
Journal of medicinal chemistry
|
Anti-HIV drugs.
|
De Clercq E
|
2007
|
Verhandelingen - Koninklijke Academie voor Geneeskunde van België
|
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
|
De Clercq E
|
2007
|
Antimicrobial agents and chemotherapy
|
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.
|
De Clercq E
|
2007
|
Journal of virology
|
Ribavirin and mycophenolic acid markedly potentiate the anti-hepatitis B virus activity of entecavir.
|
De Clercq E
|
2007
|
Antiviral research
|
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
|
De Clercq E
|
2007
|
Bioorganic & medicinal chemistry letters
|
Nitroimidazoles. V. Synthesis and anti-HIV evaluation of new 5-substituted piperazinyl-4-nitroimidazole derivatives.
|
De Clercq E
|
2007
|
Acta pharmaceutica (Zagreb, Croatia)
|
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.
|
De Clercq E
|
2007
|
Journal of medicinal chemistry
|
DNA polymerase mutations in drug-resistant herpes simplex virus mutants determine in vivo neurovirulence and drug-enzyme interactions.
|
De Clercq E
|
2007
|
Antivir Ther
|
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.
|
De Clercq E
|
2007
|
European journal of medicinal chemistry
|
Synthesis of novel derivatives of 4-amino-3-(2-furyl)-5-mercapto-1,2,4-triazole as potential HIV-1 NNRTIs.
|
De Clercq E
|
2007
|
Molecules (Basel, Switzerland)
|
Nitroimidazoles, part 2: Synthesis, antiviral and antitumor activity of new 4-nitroimidazoles.
|
De Clercq E
|
2006
|
Chemistry & biodiversity
|
Non-nucleoside HIV-1 reverse transcriptase inhibitors, Part 7. Synthesis, antiviral activity, and 3D-QSAR investigations of novel 6-(1-naphthoyl) HEPT analogues.
|
De Clercq E
|
2006
|
Chemical & pharmaceutical bulletin
|
Cidofovir resistance in vaccinia virus is linked to diminished virulence in mice.
|
De Clercq E
|
2006
|
Journal of virology
|
Replacement of the metabolically labile methyl esters in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors with isoxazolone, isoxazole, oxazolone, or cyano substituents.
|
De Clercq E
|
2006
|
Journal of medicinal chemistry
|
Antiviral properties of new arylsulfone derivatives with activity against human betaherpesviruses.
|
De Clercq E
|
2006
|
Antiviral research
|
Synthesis and anti-HIV activity of new alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors (NNRTIs) incorporating benzoxazolone and benzisoxazole rings.
|
De Clercq E
|
2006
|
Bioorganic & medicinal chemistry
|
Synthesis and anti-HIV-1 and anti-HCMV activity of 1-substituted 3-(3,5-dimethylbenzyl)uracil derivatives.
|
De Clercq E
|
2006
|
Chemical & pharmaceutical bulletin
|
Marked depletion of glycosylation sites in HIV-1 gp120 under selection pressure by the mannose-specific plant lectins of Hippeastrum hybrid and Galanthus nivalis.
|
De Clercq E
|
2005
|
Molecular pharmacology
|
Antiadenovirus activities of several classes of nucleoside and nucleotide analogues.
|
De Clercq E
|
2005
|
Antimicrobial agents and chemotherapy
|
Susceptibilities of several clinical varicella-zoster virus (VZV) isolates and drug-resistant VZV strains to bicyclic furano pyrimidine nucleosides.
|
De Clercq E
|
2005
|
Antimicrobial agents and chemotherapy
|
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.
|
De Clercq E
|
2005
|
Molecular pharmacology
|
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.
|
De Clercq E
|
2005
|
FEBS letters
|
The role of Thr139 in the human immunodeficiency virus type 1 reverse transcriptase sensitivity to (+)-calanolide A.
|
De Clercq E
|
2005
|
Molecular pharmacology
|
First synthesis and evaluation of the inhibitory effects of aza analogues of TSAO on HIV-1 replication.
|
De Clercq E
|
2005
|
Journal of medicinal chemistry
|
(E)-5-(2-bromovinyl)-2'-deoxyuridine (BVDU).
|
De Clercq E
|
2005
|
Medicinal research reviews
|
Resistance of human immunodeficiency virus type 1 to the high-mannose binding agents cyanovirin N and concanavalin A.
|
De Clercq E
|
2005
|
Journal of virology
|
Antiviral drug discovery and development: where chemistry meets with biomedicine.
|
De Clercq E
|
2005
|
Antiviral research
|
Synthesis, anti-HIV activity, and metabolic stability of new alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
2005
|
Journal of medicinal chemistry
|
Emerging anti-HIV drugs.
|
De Clercq E
|
2005
|
Expert Opin Emerg Drugs
|
Nonnucleoside HIV-1 reverse-transcriptase inhibitors, part 5. Synthesis and anti-HIV-1 activity of novel 6-naphthylthio HEPT analogues.
|
De Clercq E
|
2005
|
Chemical & pharmaceutical bulletin
|
Deoxythreosyl phosphonate nucleosides as selective anti-HIV agents.
|
De Clercq E
|
2005
|
Journal of the American Chemical Society
|
Non-nucleoside HIV reverse transcriptase inhibitors, Part 6[1]: synthesis and anti-HIV activity of novel 2-[(arylcarbonylmethyl)thio]-6-arylthio DABO analogues.
|
De Clercq E
|
2005
|
Archiv der Pharmazie
|
Pyridine N-oxide derivatives: unusual anti-HIV compounds with multiple mechanisms of antiviral action.
|
De Clercq E
|
2005
|
The Journal of antimicrobial chemotherapy
|
Design, synthesis, anti-HIV activities, and metabolic stabilities of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
2004
|
Journal of medicinal chemistry
|
Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future.
|
De Clercq E
|
2004
|
Chemistry & biodiversity
|
Antiviral drugs in current clinical use.
|
De Clercq E
|
2004
|
J Clin Virol
|
Human herpesvirus 6 DNA polymerase: enzymatic parameters, sensitivity to ganciclovir and determination of the role of the A961V mutation in HHV-6 ganciclovir resistance.
|
De Clercq E
|
2004
|
Antiviral Res
|
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.
|
De Clercq E
|
2004
|
Bioorganic & medicinal chemistry letters
|
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.
|
De Clercq E
|
2004
|
Journal of virology
|
Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
|
De Clercq E
|
2004
|
Farmaco (Società chimica italiana : 1989)
|
Susceptibility of feline immunodeficiency virus/human immunodeficiency virus type 1 reverse transcriptase chimeras to non-nucleoside RT inhibitors.
|
De Clercq E
|
2004
|
Molecular pharmacology
|
Novel inhibitors of HIV-1 integration.
|
De Clercq E
|
2004
|
Current drug metabolism
|
Discovery and development of BVDU (brivudin) as a therapeutic for the treatment of herpes zoster.
|
De Clercq E
|
2004
|
Biochemical pharmacology
|
CADA, a novel CD4-targeted HIV inhibitor, is synergistic with various anti-HIV drugs in vitro.
|
De Clercq E
|
2004
|
AIDS (London, England)
|
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.
|
De Clercq E
|
2004
|
Bioorganic chemistry
|
2-(2,6-Dihalophenyl)-3-(pyrimidin-2-yl)-1,3-thiazolidin-4-ones as non-nucleoside HIV-1 reverse transcriptase inhibitors.
|
De Clercq E
|
2004
|
Antiviral research
|
In vitro selection of drug-resistant varicella-zoster virus (VZV) mutants (OKA strain): differences between acyclovir and penciclovir?
|
De Clercq E
|
2004
|
Antiviral research
|
Synthesis, solution conformation and anti-HIV activity of novel 3'-substituted-2',3'-dideoxy-5-hydroxymethyluridines and their 4,5-substituted analogues.
|
De Clercq E
|
2003
|
Antiviral chemistry & chemotherapy
|
Potent and selective inhibition of HIV and SIV by prostratin interacting with viral entry.
|
De Clercq E
|
2003
|
Antiviral chemistry & chemotherapy
|
N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action.
|
De Clercq E
|
2003
|
Journal of medicinal chemistry
|
Structure-activity relationship studies on a novel family of specific HIV-1 reverse transcriptase inhibitors.
|
De Clercq E
|
2003
|
Antiviral chemistry & chemotherapy
|
Synthesis and antiviral activity of 1,3-disubstituted uracils against HIV-1 and HCMV.
|
De Clercq E
|
2003
|
Antiviral chemistry & chemotherapy
|
Nonnucleoside HIV-1 reverse transcriptase inhibitors: Part I. Synthesis and structure-activity relationship of 1-alkoxymethyl-5-alkyl-6-naphthylmethyl uracils as HEPT analogues.
|
De Clercq E
|
2003
|
Chemical & pharmaceutical bulletin
|
Inhibition of human immunodeficiency virus by a new class of pyridine oxide derivatives.
|
De Clercq E
|
2003
|
Antimicrobial agents and chemotherapy
|
Development of a cell-based enzyme-linked immunosorbent assay for high-throughput screening of HIV type 1 entry inhibitors targeting the coreceptor CXCR4.
|
De Clercq E
|
2003
|
AIDS research and human retroviruses
|
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.
|
De Clercq E
|
2003
|
Antimicrobial agents and chemotherapy
|
Novel human immunodeficiency virus (HIV) inhibitors that have a dual mode of anti-HIV action.
|
De Clercq E
|
2003
|
Antimicrobial agents and chemotherapy
|
Anti-HIV agents: design and discovery of new potent RT inhibitors.
|
De Clercq E
|
2003
|
Farmaco (Società chimica italiana : 1989)
|
Therapy and short-term prophylaxis of poxvirus infections: historical background and perspectives.
|
De Clercq E
|
2003
|
Antiviral research
|
Characterization of the catalytic subunit of the human herpesvirus 6 (HHV-6) DNA polymerase expressed in an in vitro transcription/translation assay.
|
De Clercq E
|
2003
|
Nucleosides, nucleotides & nucleic acids
|
Synthesis and antiviral activity of some 5'-N-phthaloyl-3'-azido-2',3'-dideoxythymidine analogues.
|
De Clercq E
|
2003
|
Antiviral chemistry & chemotherapy
|
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach.
|
De Clercq E
|
2002
|
Journal of medicinal chemistry
|
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.
|
De Clercq E
|
2002
|
Antiviral research
|
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.
|
De Clercq E
|
2002
|
Journal of medical virology
|
New developments in anti-HIV chemotherapy.
|
De Clercq E
|
2002
|
Biochimica et biophysica acta
|
In search of authentic inhibitors of HIV-1 integration.
|
De Clercq E
|
2002
|
Antiviral chemistry & chemotherapy
|
Prevalence and origin of HIV-1 group M subtypes among patients attending a Belgian hospital in 1999.
|
De Clercq E
|
2002
|
Virus research
|
New class of HIV integrase inhibitors that block viral replication in cell culture.
|
De Clercq E
|
2002
|
Current biology : CB
|
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.
|
De Clercq E
|
2002
|
Molecular pharmacology
|
Highlights in the development of new antiviral agents.
|
De Clercq E
|
2002
|
Mini reviews in medicinal chemistry
|
New anti-HIV agents and targets.
|
De Clercq E
|
2002
|
Medicinal research reviews
|
Inhibition of human immunodeficiency virus type 1 integration by diketo derivatives.
|
De Clercq E
|
2002
|
Antimicrobial agents and chemotherapy
|
Identification of a novel family of nucleosides that specifically inhibit HIV-1 reverse transcriptase.
|
De Clercq E
|
2001
|
Bioorganic & medicinal chemistry letters
|
Evolution of anti-HIV drug candidates. Part 1: From alpha-anilinophenylacetamide (alpha-APA) to imidoyl thiourea (ITU).
|
De Clercq E
|
2001
|
Bioorganic & medicinal chemistry letters
|
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.
|
De Clercq E
|
2001
|
Antiviral chemistry & chemotherapy
|
Anti-HIV-1 activity of benzothiadiazine dioxide.
|
De Clercq E
|
2001
|
Antiviral chemistry & chemotherapy
|
Rapid alternation of drug therapy is highly efficient in suppressing the emergence of mutant drug-resistant HIV strains in cell culture.
|
De Clercq E
|
2001
|
AIDS research and human retroviruses
|
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.
|
De Clercq E
|
2001
|
Virology
|
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.
|
De Clercq E
|
2001
|
Journal of virology
|
Site-directed mutagenesis of human immunodeficiency virus type 1 reverse transcriptase at amino acid position 138.
|
De Clercq E
|
2001
|
Virology
|
HIV-1 integration as a target for antiretroviral therapy: a review.
|
De Clercq E
|
2001
|
Current drug targets. Infectious disorders
|
Hamao Umezawa Memorial Award Lecture: "An Odyssey in the Viral Chemotherapy Field".
|
De Clercq E
|
2001
|
International journal of antimicrobial agents
|
Inhibition of HIV infection by CXCR4 and CCR5 chemokine receptor antagonists.
|
De Clercq E
|
2001
|
Antiviral chemistry & chemotherapy
|
New developments in anti-HIV chemotherapy.
|
De Clercq E
|
2001
|
Current medicinal chemistry
|
Evaluating phenotype and genotype of drug-resistant strains in herpesviruses.
|
De Clercq E
|
2001
|
Molecular biotechnology
|
Prevalence of genotypic resistance among antiretroviral drug-naive HIV-1-infected patients in Belgium.
|
De Clercq E
|
2001
|
Antiviral therapy
|
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.
|
De Clercq E
|
2001
|
Antiviral research
|
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.
|
De Clercq E
|
2000
|
The Journal of general virology
|
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.
|
De Clercq E
|
2000
|
AIDS research and human retroviruses
|
Evaluating Clinical Isolates for Their Phenotypic and Genotypic Resistance Against Anti-HIV Drugs.
|
De Clercq E
|
2000
|
Methods in molecular medicine
|
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.
|
De Clercq E
|
2000
|
AIDS research and human retroviruses
|
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.
|
De Clercq E
|
2000
|
Molecular pharmacology
|
Anti-(herpes simplex virus) activity of 4'-thio-2'-deoxyuridines: a biochemical investigation for viral and cellular target enzymes.
|
De Clercq E
|
2000
|
The Biochemical journal
|
Ribavirin and mycophenolic acid potentiate the activity of guanine- and diaminopurine-based nucleoside analogues against hepatitis B virus.
|
De Clercq E
|
2000
|
Antiviral research
|
Novel agents for the therapy of varicella-zoster virus infections.
|
De Clercq E
|
2000
|
Expert opinion on investigational drugs
|
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.
|
De Clercq E
|
2000
|
Molecular pharmacology
|
Synthesis and anti-HIV activity of cosalane analogues incorporating nitrogen in the linker chain.
|
De Clercq E
|
2000
|
Bioorganic & medicinal chemistry
|
Current lead natural products for the chemotherapy of human immunodeficiency virus (HIV) infection.
|
De Clercq E
|
2000
|
Medicinal research reviews
|
Prevalence and characteristics of multinucleoside-resistant human immunodeficiency virus type 1 among European patients receiving combinations of nucleoside analogues.
|
De Clercq E
|
2000
|
Antimicrobial agents and chemotherapy
|
In vitro evaluation of the effect of temporary removal of HIV drug pressure.
|
De Clercq E
|
2000
|
Antiviral research
|
Fidelity analysis of HIV-1 reverse transcriptase mutants with an altered amino-acid sequence at residues Leu74, Glu89, Tyr115, Tyr183 and Met184.
|
De Clercq E
|
2000
|
European journal of biochemistry / FEBS
|
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.
|
De Clercq E
|
2000
|
Journal of viral hepatitis
|
The HIV-1 reverse transcription (RT) process as target for RT inhibitors.
|
De Clercq E
|
2000
|
Medicinal research reviews
|
Activity of non-nucleoside reverse transcriptase inhibitors against HIV-2 and SIV.
|
De Clercq E
|
1999
|
AIDS (London, England)
|
Hydroxyurea potentiates the antiherpesvirus activities of purine and pyrimidine nucleoside and nucleoside phosphonate analogs.
|
De Clercq E
|
1999
|
Antimicrobial agents and chemotherapy
|
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.
|
De Clercq E
|
1999
|
Bioorganic & medicinal chemistry
|
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.
|
De Clercq E
|
1999
|
Transplantation
|
Inhibition of human immunodeficiency virus type (HIV-1) replication by some diversely functionalized spirocyclopropyl derivatives.
|
De Clercq E
|
1999
|
Archiv der Pharmazie
|
Current pharmacological approaches to the therapy of varicella zoster virus infections: a guide to treatment.
|
De Clercq E
|
1999
|
Drugs
|
9-(2-Phosphonylmethoxyethyl)adenine induces tumor cell differentiation or cell death by blocking cell cycle progression through the S phase.
|
De Clercq E
|
1999
|
Cell growth & differentiation : the molecular biology journal of the American Association for Cancer Research
|
Role of antimetabolites of purine and pyrimidine nucleotide metabolism in tumor cell differentiation.
|
De Clercq E
|
1999
|
Biochemical pharmacology
|
Perspectives for the treatment of hepatitis B virus infections.
|
De Clercq E
|
1999
|
International journal of antimicrobial agents
|
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.
|
De Clercq E
|
1999
|
Journal of medicinal chemistry
|
An approach towards the synthesis of potential metal-chelating TSAO-T derivatives as bidentate inhibitors of human immunodeficiency virus type 1 reverse transcriptase.
|
De Clercq E
|
1998
|
Antiviral chemistry & chemotherapy
|
Treatment of visna virus infection in lambs with the acyclic nucleoside phosphonate analogue 9-(2-phosphonylmethoxyethyl)adenine (PMEA).
|
De Clercq E
|
1998
|
Antiviral chemistry & chemotherapy
|
The role of non-nucleoside reverse transcriptase inhibitors (NNRTIs) in the therapy of HIV-1 infection.
|
De Clercq E
|
1998
|
Antiviral research
|
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.
|
De Clercq E
|
1998
|
The Journal of general virology
|
The antiherpesvirus activity of H2G [(R)-9-[4-hydroxy-2-(hydroxymethyl)butyl]guanine] is markedly enhanced by the novel immunosuppressive agent mycophenolate mofetil.
|
De Clercq E
|
1998
|
Antimicrobial agents and chemotherapy
|
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.
|
De Clercq E
|
1998
|
AIDS research and human retroviruses
|
The novel immunosuppressive agent mycophenolate mofetil markedly potentiates the antiherpesvirus activities of acyclovir, ganciclovir, and penciclovir in vitro and in vivo.
|
De Clercq E
|
1998
|
Antimicrobial agents and chemotherapy
|
New perspectives for the treatment of HIV infections.
|
De Clercq E
|
1998
|
Verhandelingen - Koninklijke Academie voor Geneeskunde van België
|
Comparison of the LiPA HIV-1 RT test, selective PCR and direct solid phase sequencing for the detection of HIV-1 drug resistance mutations.
|
De Clercq E
|
1998
|
Journal of virological methods
|
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.
|
De Clercq E
|
1998
|
Antimicrobial agents and chemotherapy
|
Multiple dideoxynucleoside analogue-resistant (MddNR) HIV-1 strains isolated from patients from different European countries.
|
De Clercq E
|
1998
|
AIDS (London, England)
|
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.
|
De Clercq E
|
1998
|
Journal of medicinal chemistry
|
Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase.
|
De Clercq E
|
1998
|
Journal of medicinal chemistry
|
In search of a selective antiviral chemotherapy.
|
De Clercq E
|
1997
|
Clinical microbiology reviews
|
Sulfated polysaccharides extracted from sea algae as potential antiviral drugs.
|
De Clercq E
|
1997
|
General pharmacology
|
Reverse transcriptase fidelity and HIV-1 variation.
|
De Clercq E
|
1997
|
Science (New York, N.Y.)
|
SRR-SB3, a disulfide-containing macrolide that inhibits a late stage of the replicative cycle of human immunodeficiency virus.
|
De Clercq E
|
1997
|
Antimicrobial agents and chemotherapy
|
SIV/HIV-1 hybrid virus expressing the reverse transcriptase gene of HIV-1 remains sensitive to HIV-1-specific reverse transcriptase inhibitors after passage in rhesus macaques.
|
De Clercq E
|
1997
|
Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association
|
Models which explain the inhibition of reverse transcriptase by HIV-1-specific (thio)carboxanilide derivatives.
|
De Clercq E
|
1997
|
Biochemical and biophysical research communications
|
Zidovudine-resistant human immunodeficiency virus type 1 strains subcultured in the presence of both lamivudine and quinoxaline HBY 097 retain marked sensitivity to HBY 097 but not to lamivudine.
|
De Clercq E
|
1997
|
The Journal of infectious diseases
|
Varicella-zoster virus thymidine kinase gene and antiherpetic pyrimidine nucleoside analogues in a combined gene/chemotherapy treatment for cancer.
|
De Clercq E
|
1997
|
Gene therapy
|
Characteristics of the Pro225His mutation in human immunodeficiency virus type 1 (HIV-1) reverse transcriptase that appears under selective pressure of dose-escalating quinoxaline treatment of HIV-1.
|
De Clercq E
|
1997
|
Journal of virology
|
Development of resistance of human immunodeficiency virus (HIV) to anti-HIV agents: how to prevent the problem?
|
De Clercq E
|
1997
|
International journal of antimicrobial agents
|
Novel L-lyxo and 5'-deoxy-5'-modified TSAO-T analogs: synthesis and anti-HIV-1 activity.
|
De Clercq E
|
1996
|
Antiviral research
|
Highly favorable antiviral activity and resistance profile of the novel thiocarboxanilide pentenyloxy ether derivatives UC-781 and UC-82 as inhibitors of human immunodeficiency virus type 1 replication.
|
De Clercq E
|
1996
|
Molecular pharmacology
|
A two plasmid co-expression system in Escherichia coli for the production of virion-like reverse transcriptase of the human immunodeficiency virus type 1.
|
De Clercq E
|
1996
|
Journal of virological methods
|
Anti-HIV and anti-HBV activity and resistance profile of 2',3'-dideoxy-3'-thiacytidine (3TC) and its arylphosphoramidate derivative CF 1109.
|
De Clercq E
|
1996
|
Biochemical and biophysical research communications
|
Analysis of inhibition of retroviral reverse transcriptase.
|
De Clercq E
|
1996
|
Methods in enzymology
|
Therapeutic potential of Cidofovir (HPMPC, Vistide) for the treatment of DNA virus (i.e. herpes-, papova-, pox- and adenovirus) infections.
|
De Clercq E
|
1996
|
Verhandelingen - Koninklijke Academie voor Geneeskunde van België
|
Marked inhibitory activity of non-nucleoside reverse transcriptase inhibitors against human immunodeficiency virus type 1 when combined with (-)2',3'-dideoxy-3'-thiacytidine.
|
De Clercq E
|
1996
|
Molecular pharmacology
|
Chemical crosslinking of the subunits of HIV-1 reverse transcriptase.
|
De Clercq E
|
1996
|
Protein science : a publication of the Protein Society
|
Development of vaginal microbicides for the prevention of heterosexual transmission of HIV.
|
De Clercq E
|
1996
|
Journal of acquired immune deficiency syndromes and human retrovirology : official publication of the International Retrovirology Association
|
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) for the treatment of human immunodeficiency virus type 1 (HIV-1) infections: strategies to overcome drug resistance development.
|
De Clercq E
|
1996
|
Medicinal research reviews
|
Betulinic acid derivatives: a new class of human immunodeficiency virus type 1 specific inhibitors with a new mode of action.
|
De Clercq E
|
1996
|
Journal of medicinal chemistry
|
Betulinic acid derivatives: a new class of specific inhibitors of human immunodeficiency virus type 1 entry.
|
De Clercq E
|
1996
|
Journal of medicinal chemistry
|
Antiviral activity of the bicyclam derivative JM3100 against drug-resistant strains of human immunodeficiency virus type 1.
|
De Clercq E
|
1996
|
Antiviral research
|
New arylpyrido-diazepine and -thiodiazepine derivatives are potent and highly selective HIV-1 inhibitors targeted at the reverse transcriptase.
|
De Clercq E
|
1996
|
Antiviral research
|
Efficacy of triple combination therapy with zidovudine (ZDV) plus zalcitabine (ddC) plus lamivudine (3TC) versus double (ZDV+3TC) combination therapy in patients previously treated with ZDV+ddC.
|
De Clercq E
|
1996
|
AIDS (London, England)
|
Chemotherapy of human immunodeficiency virus (HIV) infection: anti-HIV agents targeted at early stages in the virus replicative cycle.
|
De Clercq E
|
1996
|
Biomedicine & pharmacotherapy = Biomédecine & pharmacothérapie
|
Identification of novel thiocarboxanilide derivatives that suppress a variety of drug-resistant mutant human immunodeficiency virus type 1 strains at a potency similar to that for wild-type virus.
|
De Clercq E
|
1996
|
Antimicrobial agents and chemotherapy
|
Knocking out human immunodeficiency virus through non-nucleoside reverse transcriptase inhibitors used as single agents or in combinations: a paradigm for the cure of AIDS?
|
De Clercq E
|
1995
|
Farmaco (Società chimica italiana : 1989)
|
Differential activities of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives against different human immunodeficiency virus type 1 mutant strains.
|
De Clercq E
|
1995
|
Antimicrobial agents and chemotherapy
|
Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase.
|
De Clercq E
|
1995
|
Journal of medicinal chemistry
|
Activity of various thiocarboxanilide derivatives against wild-type and several mutant human immunodeficiency virus type 1 strains.
|
De Clercq E
|
1995
|
Antiviral research
|
Sensitivity/resistance profile of a simian immunodeficiency virus containing the reverse transcriptase gene of human immunodeficiency virus type 1 (HIV-1) toward the HIV-1-specific non-nucleoside reverse transcriptase inhibitors.
|
De Clercq E
|
1995
|
Biochemical and biophysical research communications
|
Suppression of the breakthrough of human immunodeficiency virus type 1 (HIV-1) in cell culture by thiocarboxanilide derivatives when used individually or in combination with other HIV-1-specific inhibitors (i.e., TSAO derivatives).
|
De Clercq E
|
1995
|
Proceedings of the National Academy of Sciences of the United States of America
|
Antiviral therapy for human immunodeficiency virus infections.
|
De Clercq E
|
1995
|
Clinical microbiology reviews
|
Human immunodeficiency virus 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors may suppress the replication of specific drug-resistant (E138K)RT HIV-1 mutants or select for highly resistant (Y181C-->C181I)RT HIV-1 mutants.
|
De Clercq E
|
1994
|
Proceedings of the National Academy of Sciences of the United States of America
|
New tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione derivatives are potent inhibitors of human immunodeficiency virus type 1 replication and are synergistic with 2',3'-dideoxynucleoside analogs.
|
De Clercq E
|
1994
|
Antimicrobial agents and chemotherapy
|
How to overcome resistance of HIV-1 to HIV-1-specific reverse transcriptase inhibitors.
|
De Clercq E
|
1994
|
AIDS (London, England)
|
New developments in the chemotherapy of lentivirus (human immunodeficiency virus) infections: sensitivity/resistance of HIV-1 to non-nucleoside HIV-1-specific inhibitors.
|
De Clercq E
|
1994
|
Annals of the New York Academy of Sciences
|
Preclinical evaluation of MKC-442, a highly potent and specific inhibitor of human immunodeficiency virus type 1 in vitro.
|
De Clercq E
|
1994
|
Antimicrobial agents and chemotherapy
|
HIV resistance to reverse transcriptase inhibitors.
|
De Clercq E
|
1994
|
Biochemical pharmacology
|
Mechanism of action of acyclic nucleoside phosphonates against herpes virus replication.
|
De Clercq E
|
1994
|
Biochemical pharmacology
|
Resistance pattern of human immunodeficiency virus type 1 reverse transcriptase to quinoxaline S-2720.
|
De Clercq E
|
1994
|
Journal of virology
|
Resistance of HIV-1 reverse transcriptase against [2',5'-bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2''-dioxide)] (TSAO) derivatives is determined by the mutation Glu138-->Lys on the p51 subunit.
|
De Clercq E
|
1994
|
The Journal of biological chemistry
|
Sensitivity of (138 Glu-->Lys) mutated human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) to HIV-1-specific RT inhibitors.
|
De Clercq E
|
1994
|
Biochemical and biophysical research communications
|
Comparative cytostatic activity of different antiherpetic drugs against herpes simplex virus thymidine kinase gene-transfected tumor cells.
|
De Clercq E
|
1994
|
Molecular pharmacology
|
Antiviral agents: characteristic activity spectrum depending on the molecular target with which they interact.
|
De Clercq E
|
1993
|
Advances in virus research
|
Human immunodeficiency virus type 1 drug-resistance patterns with different 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives.
|
De Clercq E
|
1993
|
Molecular pharmacology
|
Inhibition of visna virus replication by 2',3'-dideoxynucleosides and acyclic nucleoside phosphonate analogs.
|
De Clercq E
|
1993
|
Antimicrobial agents and chemotherapy
|
Knocking-out concentrations of HIV-1-specific inhibitors completely suppress HIV-1 infection and prevent the emergence of drug-resistant virus.
|
De Clercq E
|
1993
|
Virology
|
Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combinations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy.
|
De Clercq E
|
1993
|
Journal of virology
|
Human immunodeficiency virus type 1-specific [2',5'-bis-O-(tert- butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"- oxathiole-2",2"-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodeficiency virus type 1-specific non-nucleoside analogues.
|
De Clercq E
|
1993
|
Molecular pharmacology
|
HIV-1-specific reverse transcriptase inhibitors show differential activity against HIV-1 mutant strains containing different amino acid substitutions in the reverse transcriptase.
|
De Clercq E
|
1993
|
Virology
|
Activity of the anti-HIV agent 9-(2-phosphonyl-methoxyethyl)-2,6-diaminopurine against cytomegalovirus in vitro and in vivo.
|
De Clercq E
|
1993
|
European journal of clinical microbiology & infectious diseases : official publication of the European Society of Clinical Microbiology
|
HIV-1-specific RT inhibitors: highly selective inhibitors of human immunodeficiency virus type 1 that are specifically targeted at the viral reverse transcriptase.
|
De Clercq E
|
1993
|
Medicinal research reviews
|
Kinetics of different human immunodeficiency virus type 1 reverse transcriptases resistant to human immunodeficiency virus type 1-specific reverse transcriptase inhibitors.
|
De Clercq E
|
1993
|
Molecular pharmacology
|
[Highly specific inhibitors of human immunodeficiency virus type I that are particularly targeted at the reverse transcriptase].
|
De Clercq E
|
1993
|
Pathologie-biologie
|
Differential inhibitory effects of TIBO derivatives on different strains of simian immunodeficiency virus.
|
De Clercq E
|
1992
|
The Journal of general virology
|
Resistance of human immunodeficiency virus type 1 reverse transcriptase to TIBO derivatives induced by site-directed mutagenesis.
|
De Clercq E
|
1992
|
Virology
|
Common features in the interaction of tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives with the human immunodeficiency virus type 1 reverse transcriptase.
|
De Clercq E
|
1992
|
Molecular pharmacology
|
HIV inhibitors targeted at the reverse transcriptase.
|
De Clercq E
|
1992
|
AIDS research and human retroviruses
|
New perspectives for the chemotherapy and chemoprophylaxis of AIDS (acquired immune deficiency syndrome).
|
De Clercq E
|
1992
|
Verhandelingen - Koninklijke Academie voor Geneeskunde van België
|
Specific HIV-1 reverse transcriptase inhibitors.
|
De Clercq E
|
1992
|
Journal of enzyme inhibition
|
Mechanism of anti-human immunodeficiency virus action of polyoxometalates, a class of broad-spectrum antiviral agents.
|
De Clercq E
|
1992
|
Molecular pharmacology
|
3'-C-branched 2'-deoxy-5-methyluridines: synthesis, enzyme inhibition, and antiviral properties.
|
De Clercq E
|
1992
|
Journal of medicinal chemistry
|
Anti-human immunodeficiency virus effects of cationic metalloporphyrin-ellipticine complexes.
|
De Clercq E
|
1992
|
Biochemical pharmacology
|
Kinetics of inhibition of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase by the novel HIV-1-specific nucleoside analogue [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5 "- (4"-amino-1",2"-oxathiole-2",2"-dioxide)thymine (TSAO-T).
|
De Clercq E
|
1992
|
The Journal of biological chemistry
|
2',5'-Bis-O-(tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1'',2''- oxathiole-2'',2'-dioxide)pyrimidine (TSAO) nucleoside analogues: highlyselective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase.
|
De Clercq E
|
1992
|
Proceedings of the National Academy of Sciences of the United States of America
|
[2',5'-Bis-O-(tert-butyldimethylsilyl)]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide) (TSAO) derivatives of purine and pyrimidinenucleosides as potent and selective inhibitors of human immunodeficiency virus type 1.
|
De Clercq E
|
1992
|
Antimicrobial agents and chemotherapy
|
Allosteric inhibition of human immunodeficiency virus type 1 reverse transcriptase by tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-one and -thione compounds.
|
De Clercq E
|
1992
|
Molecular pharmacology
|
Kinetics of inhibition of endogenous human immunodeficiency virus type 1 reverse transcription by 2',3'-dideoxynucleoside 5'-triphosphate, tetrahydroimidazo-[4,5,1-jk][1,4]-benzodiazepin-2(1H)-thion e, and 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine derivatives.
|
De Clercq E
|
1992
|
The Journal of biological chemistry
|
Synthesis and anti-HIV activities of low molecular weight aurintricarboxylic acid fragments and related compounds.
|
De Clercq E
|
1991
|
Journal of medicinal chemistry
|
An antiviral target on reverse transcriptase of human immunodeficiency virus type 1 revealed by tetrahydroimidazo-[4,5,1-jk] [1,4]benzodiazepin-2 (1H)-one and -thione derivatives.
|
De Clercq E
|
1991
|
Proceedings of the National Academy of Sciences of the United States of America
|
Inhibition of the growth of Plasmodium falciparum and Plasmodium berghei by the DNA polymerase inhibitor HPMPA.
|
De Clercq E
|
1991
|
Mol Biochem Parasitol
|
Intracellular metabolism and mechanism of anti-retrovirus action of 9-(2-phosphonylmethoxyethyl)adenine, a potent anti-human immunodeficiency virus compound.
|
De Clercq E
|
1991
|
Proceedings of the National Academy of Sciences of the United States of America
|
9-[(2RS)-3-fluoro-2-phosphonylmethoxypropyl] derivatives of purines: a class of highly selective antiretroviral agents in vitro and in vivo.
|
De Clercq E
|
1991
|
Proceedings of the National Academy of Sciences of the United States of America
|
Highly potent and selective inhibition of human immunodeficiency virus type 1 by a novel series of 6-substituted acyclouridine derivatives.
|
De Clercq E
|
1991
|
Molecular pharmacology
|
Potent and selective inhibition of human immunodeficiency virus type 1 (HIV-1) by 5-ethyl-6-phenylthiouracil derivatives through their interaction with the HIV-1 reverse transcriptase.
|
De Clercq E
|
1991
|
Proceedings of the National Academy of Sciences of the United States of America
|
Chemotherapy of the acquired immune deficiency syndrome (AIDS): acyclic nucleoside phosphonate analogues.
|
De Clercq E
|
1991
|
International journal of immunopharmacology
|
Chemotherapy of the acquired immune deficiency syndrome (AIDS): non-nucleoside inhibitors of the human immunodeficiency virus type 1 reverse transcriptase.
|
De Clercq E
|
1991
|
International journal of immunopharmacology
|
Preparation and anti-HIV activities of aurintricarboxylic acid fractions and analogues: direct correlation of antiviral potency with molecular weight.
|
De Clercq E
|
1991
|
Journal of medicinal chemistry
|
Differential inhibition of retroviral reverse transcriptase by poly(2-fluoroadenylic acid), a template analogue.
|
De Clercq E
|
1991
|
AIDS (London, England)
|
5-Phosphoribosyl 1-pyrophosphate synthetase converts the acyclic nucleoside phosphonates 9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine and 9-(2-phosphonylmethoxyethyl)adenine directly to their antivirally active diphosphate derivatives.
|
De Clercq E
|
1991
|
The Journal of biological chemistry
|
Mechanism of action of 5-(2-chloroethyl)-2'-deoxyuridine, a selective inhibitor of herpes simplex virus replication.
|
De Clercq E
|
1990
|
Molecular pharmacology
|
Selective virus inhibitors.
|
De Clercq E
|
1990
|
Microbiologica
|
Targets and strategies for the antiviral chemotherapy of AIDS.
|
De Clercq E
|
1990
|
Trends in pharmacological sciences
|
Potent inhibitory effects of the 5'-triphosphates of (E)-5-(2-bromovinyl)-2'-deoxyuridine and (E)-5-(2-bromovinyl)-1-beta-D-arabinofuranosyluracil on DNA polymerase gamma.
|
De Clercq E
|
1990
|
Eur J Biochem
|
Tumor necrosis factor enhances replication of human immunodeficiency virus (HIV) in vitro.
|
De Clercq E
|
1989
|
Biochemical and biophysical research communications
|
Potential drugs for the treatment of AIDS.
|
De Clercq E
|
1989
|
The Journal of antimicrobial chemotherapy
|
Selective activity of several cholic acid derivatives against human immunodeficiency virus replication in vitro.
|
De Clercq E
|
1989
|
Journal of acquired immune deficiency syndromes
|
Flow cytometric method to demonstrate whether anti-HIV-1 agents inhibit virion binding to T4+ cells.
|
De Clercq E
|
1989
|
Journal of acquired immune deficiency syndromes
|
Differential inhibitory effects of several pyrimidine 2',3'-dideoxynucleoside 5'-triphosphates on the activities of reverse transcriptase and various cellular DNA polymerases.
|
De Clercq E
|
1989
|
Molecular pharmacology
|
Highly specific inhibition of human immunodeficiency virus type 1 by a novel 6-substituted acyclouridine derivative.
|
De Clercq E
|
1989
|
Biochemical and biophysical research communications
|
Mechanism of inhibition of adenovirus DNA replication by the acyclic nucleoside triphosphate analogue (S)-HPMPApp: influence of the adenovirus DNA binding protein.
|
De Clercq E
|
1989
|
Nucleic acids research
|
Treatment of bovine leukaemia virus-infected sheep with suramin: an animal model for the development of antiretroviral compounds.
|
De Clercq E
|
1989
|
Acta virologica
|
Differential inhibition of various deoxyribonucleic acid polymerases by Evans blue and aurintricarboxylic acid.
|
De Clercq E
|
1988
|
European journal of biochemistry / FEBS
|
Inhibitory activity of (E)-5-(2-bromovinyl)-2'-deoxyuridine on the salmonid herpesviruses, Oncorhynchus masou virus (OMV) and Herpesvirus salmonis.
|
De Clercq E
|
1988
|
Microbiology and immunology
|
Perspectives for the chemotherapy of AIDS.
|
De Clercq E
|
1988
|
Chemioterapia : international journal of the Mediterranean Society of Chemotherapy
|
Fuchsin acid selectively inhibits human immunodeficiency virus (HIV) replication in vitro.
|
De Clercq E
|
1988
|
Biochemical and biophysical research communications
|
Mechanism of inhibitory effect of dextran sulfate and heparin on replication of human immunodeficiency virus in vitro.
|
De Clercq E
|
1988
|
Proceedings of the National Academy of Sciences of the United States of America
|
Alpha, beta- and beta, gamma-methylene 5'-phosphonate derivatives of 3'-azido-2',3'-dideoxythymidine-5'-triphosphate. Correlation between affinity for reverse transcriptase, susceptibility to hydrolysis by phosphodiesterases and anti-retrovirus activity.
|
De Clercq E
|
1988
|
Biochemical pharmacology
|
Inhibitory effect of glycyrrhizin on the in vitro infectivity and cytopathic activity of the human immunodeficiency virus [HIV (HTLV-III/LAV)].
|
De Clercq E
|
1987
|
Antiviral research
|
Phosphorylation of nucleoside analogs by equine herpesvirus type 1 pyrimidine deoxyribonucleoside kinase.
|
De Clercq E
|
1987
|
Antiviral research
|
Suramin in the treatment of AIDS: mechanism of action.
|
De Clercq E
|
1987
|
Antiviral research
|
Incorporation of the carbocyclic analogue of (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-triphosphate into a synthetic DNA.
|
De Clercq E
|
1987
|
Biochemical and biophysical research communications
|
Glycosylation inhibitors block the expression of LAV/HTLV-III (HIV) glycoproteins.
|
De Clercq E
|
1986
|
Biochemical and biophysical research communications
|
Aurintricarboxylic acid and Evans Blue represent two different classes of anionic compounds which selectively inhibit the cytopathogenicity of human T-cell lymphotropic virus type III/lymphadenopathy-associated virus.
|
De Clercq E
|
1986
|
Biochemical and biophysical research communications
|
Comparative inhibitory effects of suramin and other selected compounds on the infectivity and replication of human T-cell lymphotropic virus (HTLV-III)/lymphadenopathy-associated virus (LAV).
|
De Clercq E
|
1986
|
International journal of cancer. Journal international du cancer
|
Inhibitors of reverse transcriptase and retrovirus replication.
|
De Clercq E
|
1985
|
Arzneimittel-Forschung
|
Inhibition of human and woodchuck hepatitis virus DNA polymerase by the triphosphates of acyclovir, 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)-5-iodocytosine and E-5-(2-bromovinyl)-2'-deoxyuridine.
|
De Clercq E
|
1984
|
Antiviral Res
|
Comparative inhibition of DNA polymerases from varicella zoster virus (TK+ and TK-) strains by (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-triphosphate.
|
De Clercq E
|
1984
|
Molecular pharmacology
|
Synthesis and antiviral properties of 5-vinylpyrimidine nucleoside analogs.
|
De Clercq E
|
1984
|
Pharmacology & therapeutics
|
Antiviral activity of the 3'-amino derivative of (E)-5-(2-bromovinyl)-2'-deoxyuridine.
|
De Clercq E
|
1983
|
The Biochemical journal
|
Baculovirus replication: inhibition of Trichoplusia ni multiple nuclear polyhedrosis virus by [E]-5-(2-bromovinyl)-2'-deoxyuridine.
|
De Clercq E
|
1983
|
The Journal of general virology
|
Inhibition of terminal deoxynucleotidyltransferase by (E)-5-(2-bromovinyl)-2'-deoxyuridine 5'-triphosphate.
|
De Clercq E
|
1983
|
Nucleic acids symposium series
|
Inhibition of murine leukaemia virus reverse transcriptase by 2-halogenated polyadenylic acids.
|
De Clercq E
|
1982
|
The Biochemical journal
|
Inhibitory effect of E-5-(2-bromovinyl)-1-beta-D-arabinofuranosyluracil on herpes simplex virus replication and DNA synthesis.
|
De Clercq E
|
1982
|
Journal of virology
|
On the mechanism of selective inhibition of herpesvirus replication by (E)-5-(2-bromovinyl)-2'-deoxyuridine.
|
De Clercq E
|
1981
|
Proceedings of the National Academy of Sciences of the United States of America
|
Influence of various 2- and 2'-substituted polyadenylic acids on murine leukemia virus reverse transcriptase.
|
De Clercq E
|
1979
|
Cancer letters
|
Suramin: a potent inhibitor of the reverse transcriptase of RNA tumor viruses.
|
De Clercq E
|
1979
|
Cancer letters
|
Gliotoxin analogues as inhibitors of reverse transcriptase. 2. Resolution and X-ray crystal structure determination.
|
De Clercq E
|
1978
|
Journal of medicinal chemistry
|
Gliotoxin analogues as inhibitors of reverse transcriptase. 1. Effect of lipophilicity.
|
De Clercq E
|
1978
|
Journal of medicinal chemistry
|
Interferon induction by polynucleotides: structure-function relationship.
|
De Clercq E
|
1977
|
Texas reports on biology and medicine
|
Biologic activities of poly (2-azaadenylic acid) and poly (2-azainosinic acid).
|
De Clercq E
|
1977
|
Nucleic acids research
|
Role of purine N-3 in the biologic activities of poly(A) and poly(I).
|
De Clercq E
|
1976
|
Nucleic acids research
|
Inhibition of oncornavirus functions by poly (2-methylthioinosinic acid).
|
De Clercq E
|
1975
|
Nucleic acids research
|
Inhibition of oncornavirus functions by 2'-azido polynucleotides.
|
De Clercq E
|
1975
|
Proceedings of the National Academy of Sciences of the United States of America
|
Proceedings: Inhibition of mouse leukemia virus RNA-dependent DNA polymerase by 2'-OH-substituted polynucleotides.
|
De Clercq E
|
1974
|
Hoppe-Seyler's Zeitschrift für physiologische Chemie
|
A more sensitive assay system for the detection of RNA-dependent DNA polymerase in oncogenic RNA viruses.
|
De Clercq E
|
1973
|
Biochimica et biophysica acta
|