Novel Benzophenones as Non-nucleoside Reverse Transcriptase Inhibitors of HIV-1

• Published in: Journal of medicinal chemistry 2004-02, Vol.47 (5), p.1175-1182
• Main Authors: Chan, Joseph H, Freeman, George A, Tidwell, Jeffrey H, Romines, Karen R, Schaller, Lee T, Cowan, Jill R, Gonzales, Steve S, Lowell, Gina S, Andrews, C. W, Reynolds, David J, St Clair, Marty, Hazen, Richard J, Ferris, Rob G, Creech, Katrina L, Roberts, Grace B, Short, Steven A, Weaver, Kurt, Koszalka, George W, Boone, Lawrence R
• Format: Article
• Language: English
• Subjects: Anti-HIV Agents - chemical synthesis; Anti-HIV Agents - chemistry; Anti-HIV Agents - pharmacology; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antiviral agents; Benzophenones - chemical synthesis; Benzophenones - chemistry; Benzophenones - pharmacology; Biological and medical sciences; Cell Line; Crystallography, X-Ray; Drug Resistance, Viral; HIV Reverse Transcriptase - antagonists & inhibitors; HIV Reverse Transcriptase - chemistry; HIV Reverse Transcriptase - metabolism; HIV-1 - drug effects; HIV-1 - enzymology; HIV-1 - genetics; Humans; Inhibitory Concentration 50; Medical sciences; Mutation; Pharmacology. Drug treatments; Protein Binding; Reverse Transcriptase Inhibitors - chemical synthesis; Reverse Transcriptase Inhibitors - chemistry; Reverse Transcriptase Inhibitors - pharmacology; Structure-Activity Relationship
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/jm030255y

GW4511, GW4751, and GW3011 showed IC50 values ≤2 nM against wild type HIV-1 and