Erik De Clercq

发表

Synthesis, conformational analysis and antiviral and antitumoral activity of new 1,2-disubstituted carbocyclic nucleosides.

Jan Balzarini, Lourdes Santana, Marta Teijeira, 2002, European journal of medicinal chemistry.

Non-nucleoside reverse transcriptase inhibitors (NNRTIs): past, present, and future.

E. De Clercq, Erik De Clercq, 2004, Chemistry & biodiversity.

Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends.

Peng Zhan, Christophe Pannecouque, E. De Clercq, 2016, Journal of medicinal chemistry.

Structural modifications of CH(OH)-DAPYs as new HIV-1 non-nucleoside reverse transcriptase inhibitors.

Christophe Pannecouque, E. De Clercq, C. Pannecouque, 2014, Bioorganic & medicinal chemistry.

2‐(2,6‐Dihalo‐phenyl)‐3‐heteroaryl‐2‐ylmethyl‐1, 3‐thiazolidin‐4‐ones: Anti‐HIV agents

Ravindra K Rawal, Christophe Pannecouque, E. De Clercq, 2008, Chemical biology & drug design.

Non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 11: structural modulations of diaryltriazines with potent anti-HIV activity.

Jan Balzarini, Christophe Pannecouque, E. De Clercq, 2008, European journal of medicinal chemistry.

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.

Myriam Witvrouw, Jean-Jacques Vasseur, Christophe Pannecouque, 2002, Farmaco.

AMD3100, a Potent and Specific Antagonist of the Stromal Cell-Derived Factor-1 Chemokine Receptor CXCR4, Inhibits Autoimmune Joint Inflammation in IFN-γ Receptor-Deficient Mice1

Dominique Schols, E. De Clercq, A. Billiau, 2001, The Journal of Immunology.

Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.

Peng Zhan, Ye Tian, Dongwei Kang, 2017, European journal of medicinal chemistry.

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.

Peng Zhan, Jing Zhang, Christophe Pannecouque, 2011, Bioorganic & medicinal chemistry.

Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.

Peng Zhan, Jian Zhang, F. J. Luque, 2019, Journal of medicinal chemistry.

New anti-HIV agents and targets.

E. De Clercq, Erik De Clercq, 2002, Medicinal research reviews.

The design of drugs for HIV and HCV.

E. De Clercq, Erik De Clercq, 2007, Nature reviews. Drug discovery.

HIV-chemotherapy and -prophylaxis: new drugs, leads and approaches.

E. De Clercq, Erik De Clercq, 2004, The international journal of biochemistry & cell biology.

Antivirals and antiviral strategies.

E. De Clercq, Erik De Clercq, 2004, Nature reviews. Microbiology.

Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-ones.

Angela Rao, Maria Zappalà, Pietro Monforte, 2003, Farmaco.

Mutations at the CXCR4 interaction sites for AMD3100 influence anti‐CXCR4 antibody binding and HIV‐1 entry

Dominique Schols, E. De Clercq, T. Schwartz, 2003, FEBS letters.

Heparin-Mimicking Sulfonic Acid Polymers as Multitarget Inhibitors of Human Immunodeficiency Virus Type 1 Tat and gp120 Proteins

Marco Rusnati, Antonella Bugatti, E. De Clercq, 2007, Antimicrobial Agents and Chemotherapy.

Configurationally restricted bismacrocyclic CXCR4 receptor antagonists.

Stephen J Archibald, Peter J Sadler, Christophe Pannecouque, 2006, Journal of medicinal chemistry.

Twenty-six years of anti-HIV drug discovery: where do we stand and where do we go?

Youcef Mehellou, E. De Clercq, Y. Mehellou, 2010, 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.

Peng Zhan, Ye Tian, Xuwang Chen, 2012, Bioorganic & medicinal chemistry letters.

Arylazolyl(azinyl)thioacetanilides. Part 10: design, synthesis and biological evaluation of novel substituted imidazopyridinylthioacetanilides as potent HIV-1 inhibitors.

Peng Zhan, Jan Balzarini, Xuwang Chen, 2012, Bioorganic & medicinal chemistry.

Inhibition of Human Immunodeficiency Virus Replication by a Dual CCR5/CXCR4 Antagonist

Dominique Schols, E. De Clercq, T. Schwartz, 2004, Journal of Virology.

Sulfanyltriazole/tetrazoles: a promising class of HIV-1 NNRTIs.

Peng Zhan, E. De Clercq, P. Zhan, 2009, Mini reviews in medicinal chemistry.

DNA-induced Polymerization of HIV-1 Integrase Analyzed with Fluorescence Fluctuation Spectroscopy*

Jo Vercammen, Zeger Debyser, Yves Engelborghs, 2002, The Journal of Biological Chemistry.

Overview of Recent Strategic Advances in Medicinal Chemistry.

Peng Zhan, Yuning Song, Dongwei Kang, 2019, Journal of medicinal chemistry.

Multivalent agents: a novel concept and preliminary practice in Anti-HIV drug discovery.

Peng Zhan, Yu'ning Song, Erik De Clercq, 2013, Current medicinal chemistry.

Synthesis and Biological Evaluation of a Series of 2‐((1‐substituted‐1H‐1,2,3‐triazol‐4‐yl)methylthio)‐6‐(naphthalen‐1‐ylmethyl)pyrimidin‐4(3H)‐one As Potential HIV‐1 Inhibitors

Peng Zhan, Dongwei Kang, Christophe Pannecouque, 2015, Chemical biology & drug design.

Discovery and Characterization of Fluorine-Substituted Diarylpyrimidines Derivatives as Novel HIV-1 NNRTIs with Highly Improved Resistance Profiles and Low Activity for the hERG Ion Channel.

Peng Zhan, Dongwei Kang, Yanying Sun, 2020, Journal of medicinal chemistry.

Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.

Peng Zhan, Xiao Ding, Dongwei Kang, 2016, Journal of medicinal chemistry.

Discovery of novel diarylpyrimidines as potent HIV NNRTIs via a structure-guided core-refining approach.

Peng Zhan, Jan Balzarini, Ye Tian, 2014, European journal of medicinal chemistry.

Arylazolyl(azinyl)thioacetanilides. Part 16: Structure-based bioisosterism design, synthesis and biological evaluation of novel pyrimidinylthioacetanilides as potent HIV-1 inhibitors.

Peng Zhan, Jan Balzarini, Christophe Pannecouque, 2014, Bioorganic & medicinal chemistry.

ANN-QSAR model for selection of anticancer leads from structurally heterogeneous series of compounds.

Rafael Bello, Isis Bonet, Lourdes Santana, 2007, European journal of medicinal chemistry.

Design strategies of novel NNRTIs to overcome drug resistance.

Peng Zhan, Christophe Pannecouque, E. De Clercq, 2009, Current medicinal chemistry.

Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.

Peng Zhan, Xuwang Chen, Christophe Pannecouque, 2012, Bioorganic & medicinal chemistry.

Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.

Peng Zhan, Jan Balzarini, Christophe Pannecouque, 2013, Bioorganic & medicinal chemistry.

Emerging antiviral drugs.

Erik De Clercq, 2008, Expert opinion on emerging drugs.

Recent advances in antiviral activity of benzo/heterothiadiazine dioxide derivatives.

Peng Zhan, E. De Clercq, P. Zhan, 2008, Current medicinal chemistry.

Synthesis and Studies of New 2‐(Coumarin‐4‐yloxy)‐4,6‐(substituted)‐s‐Triazine Derivatives as Potential Anti‐HIV Agents

Christophe Pannecouque, E. De Clercq, C. Pannecouque, 2009, Archiv der Pharmazie.

Design, synthesis, and biologic evaluation of novel galloyl derivatives as HIV‐1 RNase H inhibitors

Peng Zhan, Jacob Kongsted, Luis Menéndez-Arias, 2019, Chemical biology & drug design.

Design and synthesis of bioactive adamantane spiro heterocycles.

Lieve Naesens, Grigoris Zoidis, George Fytas, 2007, Bioorganic & medicinal chemistry letters.

Design, synthesis and preliminary SAR studies of novel N-arylmethyl substituted piperidine-linked aniline derivatives as potent HIV-1 NNRTIs.

Peng Zhan, Jan Balzarini, Xuwang Chen, 2014, Bioorganic & medicinal chemistry.

Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-(thi)one derivatives.

Angela Rao, Maria Zappalà, Pietro Monforte, 2002, Farmaco.

Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.

Peng Zhan, E. De Clercq, P. Zhan, 2012, Journal of medicinal chemistry.

Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach.

Peng Zhan, Ye Tian, Christophe Pannecouque, 2014, European journal of medicinal chemistry.

Diverging binding capacities of natural LD78β isoforms of macrophage inflammatory protein‐1α to the CC chemokine receptors 1, 3 and 5 affect their anti‐HIV‐1 activity and chemotactic potencies for neutrophils and eosinophils

Dominique Schols, Paul Proost, E. De Clercq, 2001, European journal of immunology.

Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents.

Jan Balzarini, Angela Rao, Maria Zappalà, 2004, Farmaco.

Strategies in the design of antiviral drugs

E. De Clercq, Erik De Clercq, 2002, Nature reviews. Drug discovery.

Design, synthesis and biological evaluation of N2,N4-disubstituted-1,1,3-trioxo-2H,4H-pyrrolo[1,2-b][1,2,4,6]thiatriazine derivatives as HIV-1 NNRTIs.

Peng Zhan, Jan Balzarini, Christophe Pannecouque, 2013, Bioorganic & medicinal chemistry.

Fused heterocyclic compounds bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 1: design, synthesis and biological evaluation of novel 5,7-disubstituted pyrazolo[1,5-a]pyrimidine derivatives.

Peng Zhan, Ye Tian, Christophe Pannecouque, 2014, Bioorganic & medicinal chemistry.

Spiro[pyrrolidine-2,2'-adamantanes]: synthesis, anti-influenza virus activity and conformational properties.

Antonios Kolocouris, Johan Neyts, George Fytas, 2003, Bioorganic & medicinal chemistry letters.

Synthesis of new covalently bound kappa-carrageenan-AZT conjugates with improved anti-HIV activities.

Myriam Witvrouw, Christophe Pannecouque, Jean-Louis Kraus, 2002, Journal of medicinal chemistry.

QSAR for anti-RNA-virus activity, synthesis, and assay of anti-RSV carbonucleosides given a unified representation of spectral moments, quadratic, and topologic indices.

Maykel Cruz-Monteagudo, Lourdes Santana, Humberto González-Díaz, 2005, Bioorganic & medicinal chemistry letters.

Potential antivirals and antiviral strategies against SARS coronavirus infections

E. De Clercq, Erik De Clercq, 2006, Expert review of anti-infective therapy.

Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.

Peng Zhan, Jan Balzarini, Christophe Pannecouque, 2014, Bioorganic & medicinal chemistry.

Computational strategies in discovering novel non-nucleoside inhibitors of HIV-1 RT.

Jan Balzarini, Angela Rao, Maria Zappalà, 2005, Journal of medicinal chemistry.

Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.

Peng Zhan, Jan Balzarini, Xuwang Chen, 2012, European journal of medicinal chemistry.

The novel C-5 aryl, alkenyl, and alkynyl substituted uracil derivatives of L-ascorbic acid: synthesis, cytostatic, and antiviral activity evaluations.

Jan Balzarini, Marko Marjanović, E. De Clercq, 2007, Bioorganic & medicinal chemistry.

Cytotoxic analogues of 2,6-bis(arylidene)cyclohexanones.

Jan Balzarini, James P Stables, Theresa M Allen, 2003, European journal of medicinal chemistry.

Design and synthesis of 2-(2,6-dibromophenyl)-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.

Ravindra K Rawal, Christophe Pannecouque, E. De Clercq, 2008, European journal of medicinal chemistry.

Synthesis and biological activity of 4-thiazolidinones, thiosemicarbazides derived from diflunisal hydrazide.

Erik De Clercq, Medine Güllüce, Fikrettin Sahin, 2006, European journal of medicinal chemistry.

Synthesis and biological evaluation of 2,3-diaryl substituted-1,3-thiazolidin-4-ones as anti-HIV agents.

Ravindra K Rawal, Christophe Pannecouque, E. De Clercq, 2007, Medicinal chemistry (Shariqah (United Arab Emirates)).

Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles.

Peng Zhan, F. J. Luque, Ye Tian, 2019, Journal of medicinal chemistry.

Amino-terminal Truncation of Chemokines by CD26/Dipeptidyl-peptidase IV

Dominique Schols, Paul Proost, E. De Clercq, 1998, The Journal of Biological Chemistry.

Design, synthesis, and evaluation of 2-aryl-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.

Ravindra K Rawal, Christophe Pannecouque, E. De Clercq, 2007, Bioorganic & medicinal chemistry.

Synthesis and evaluation of 2-(2,6-dihalophenyl)-3-pyrimidinyl-1,3-thiazolidin-4-one analogues as anti-HIV-1 agents.

Ravindra K Rawal, Christophe Pannecouque, E. De Clercq, 2007, Bioorganic & Medicinal Chemistry.

Synthesis of some novel heterocyclic compounds derived from diflunisal hydrazide as potential anti-infective and anti-inflammatory agents.

Ilkay Küçükgüzel, E. De Clercq, L. Kabasakal, 2007, European journal of medicinal chemistry.

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

Jan Balzarini, Anna Karlsson, E. De Clercq, 2001, Journal of Virology.

Discovery of novel DAPY-IAS hybrid derivatives as potential HIV-1 inhibitors using molecular hybridization based on crystallographic overlays.

Peng Zhan, Xueshun Wang, Christophe Pannecouque, 2017, Bioorganic & medicinal chemistry.

5-Hydroxypyrido[2,3-b]pyrazin-6(5H)-one derivatives as novel dual inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H and integrase.

Peng Zhan, Xiao Ding, Luis Menéndez-Arias, 2018, European journal of medicinal chemistry.

3,5-Bis(benzylidene)-1-[3-(2-hydroxyethylthio)propanoyl]piperidin-4-ones: a novel cluster of potent tumor-selective cytotoxins.

Jan Balzarini, Hiroshi Sakagami, E. De Clercq, 2011, Journal of medicinal chemistry.

HIV-1 Integrase Forms Stable Tetramers and Associates with LEDGF/p75 Protein in Human Cells*

Zeger Debyser, Yves Engelborghs, Bart Devreese, 2003, The Journal of Biological Chemistry.

Design, synthesis and anti-HIV evaluation of novel diarylnicotinamide derivatives (DANAs) targeting the entrance channel of the NNRTI binding pocket through structure-guided molecular hybridization.

Peng Zhan, Christophe Pannecouque, E. De Clercq, 2014, European journal of medicinal chemistry.

Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.

Dominique Schols, E. De Clercq, D. Schols, 2010, Journal of medicinal chemistry.

Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.

Peng Zhan, Xiao Ding, Ye Tian, 2017, Journal of medicinal chemistry.

AMD3465, a monomacrocyclic CXCR4 antagonist and potent HIV entry inhibitor.

Dominique Schols, E. De Clercq, T. Schwartz, 2005, Biochemical pharmacology.

Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.

Christophe Pannecouque, E. De Clercq, C. Pannecouque, 2014, Bioorganic & medicinal chemistry.

Prevalence and origin of HIV-1 group M subtypes among patients attending a Belgian hospital in 1999.

Anne-Mieke Vandamme, Inge Derdelinckx, Joke Snoeck, 2002, Virus research.

Discovery of nitropyridine derivatives as potent HIV-1 non-nucleoside reverse transcriptase inhibitors via a structure-based core refining approach.

Peng Zhan, Christophe Pannecouque, E. De Clercq, 2014, European journal of medicinal chemistry.

Antiviral agents active against influenza A viruses

E. De Clercq, Erik De Clercq, 2006, Nature reviews. Drug discovery.