Design, synthesis, and antiviral activity of a series of CD4-mimetic small-molecule HIV-1 entry inhibitors.
Bioorganic & Medicinal Chemistry
Curreli, Francesca F; Ahmed, Shahad S; Benedict Victor, Sofia M SM; Iusupov, Ildar R IR; Spiridonov, Evgeny A EA; Belov, Dmitry S DS; Altieri, Andrea A; Kurkin, Alexander V AV; Debnath, Asim K AK
Preclinical Optimization of gp120 Entry Antagonists as anti-HIV-1 Agents with Improved Cytotoxicity and ADME Properties through Rational Design, Synthesis, and Antiviral Evaluation.
Journal Of Medicinal Chemistry
Curreli, Francesca F; Ahmed, Shahad S; Benedict Victor, Sofia M SM; Iusupov, Ildar R IR; Belov, Dmitry S DS; Markov, Pavel O PO; Kurkin, Alexander V AV; Altieri, Andrea A; Debnath, Asim K AK
Selectivity for strand-transfer over 3'-processing and susceptibility to clinical resistance of HIV-1 integrase inhibitors are driven by key enzyme-DNA interactions in the active site.
Nucleic Acids Research
Métifiot, Mathieu M; Johnson, Barry C BC; Kiselev, Evgeny E; Marler, Laura L; Zhao, Xue Zhi XZ; Burke, Terrence R TR; Marchand, Christophe C; Hughes, Stephen H SH; Pommier, Yves Y
Human DDX3 protein is a valuable target to develop broad spectrum antiviral agents.
Proceedings Of The National Academy Of Sciences Of The United States Of America
Brai, Annalaura A; Fazi, Roberta R; Tintori, Cristina C; Zamperini, Claudio C; Bugli, Francesca F; Sanguinetti, Maurizio M; Stigliano, Egidio E; Esté, José J; Badia, Roger R; Franco, Sandra S; Martinez, Miguel A MA; Martinez, Javier P JP; Meyerhans, Andreas A; Saladini, Francesco F; Zazzi, Maurizio M; Garbelli, Anna A; Maga, Giovanni G; Botta, Maurizio M
HIV-1 Integrase Strand Transfer Inhibitors with Reduced Susceptibility to Drug Resistant Mutant Integrases.
Acs Chemical Biology
Zhao, Xue Zhi XZ; Smith, Steven J SJ; Maskell, Daniel P DP; Metifiot, Mathieu M; Pye, Valerie E VE; Fesen, Katherine K; Marchand, Christophe C; Pommier, Yves Y; Cherepanov, Peter P; Hughes, Stephen H SH; Burke, Terrence R TR
4-amino-1-hydroxy-2-oxo-1,8-naphthyridine-containing compounds having high potency against raltegravir-resistant integrase mutants of HIV-1.
Journal Of Medicinal Chemistry
Zhao, Xue Zhi XZ; Smith, Steven J SJ; Métifiot, Mathieu M; Marchand, Christophe C; Boyer, Paul L PL; Pommier, Yves Y; Hughes, Stephen H SH; Burke, Terrence R TR
Bicyclic 1-hydroxy-2-oxo-1,2-dihydropyridine-3-carboxamide-containing HIV-1 integrase inhibitors having high antiviral potency against cells harboring raltegravir-resistant integrase mutants.
Journal Of Medicinal Chemistry
Zhao, Xue Zhi XZ; Smith, Steven J SJ; Métifiot, Mathieu M; Johnson, Barry C BC; Marchand, Christophe C; Pommier, Yves Y; Hughes, Stephen H SH; Burke, Terrence R TR
Zhao, Xue Zhi XZ; Maddali, Kasthuraiah K; Smith, Steven J SJ; Métifiot, Mathieu M; Johnson, Barry C BC; Marchand, Christophe C; Hughes, Stephen H SH; Pommier, Yves Y; Burke, Terrence R TR