Novel Benzophenones as Non-nucleoside Reverse Transcriptase Inhibitors of HIV-1
Journal of Medicinal Chemistry2004Vol. 47(5), pp. 1175–1182
Citations Over TimeTop 14% of 2004 papers
Joseph H. Chan, George A. Freeman, Jeffrey H. Tidwell, Karen R. Romines, Lee T. Schaller, Jill R. Cowan, Steve S. Gonzales, Gina S. Lowell, C. Webster Andrews, David J. Reynolds, Marty St. Clair, Richard Hazen, Rob G. Ferris, Katrina L. Creech, Grace Roberts, Steven A. Short, Kurt Weaver, George W. Koszalka, Lawrence R. Boone
Abstract
GW4511, GW4751, and GW3011 showed IC50 values < or =2 nM against wild type HIV-1 and <10 nM against 16 mutants. They were particularly potent against NNRTI-resistant viruses containing Y181C-, K103N-, and K103N-based double mutations, which account for a significant proportion of the clinical failure of the three currently marketed NNRTIs. The antiviral data together with the favorable pharmacokinetic data of GW4511 suggested that these benzophenones possess attributes of a new NNRTI drug candidate.
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