| Literature DB >> 14971897 |
Joseph H Chan1, George A Freeman, Jeffrey H Tidwell, Karen R Romines, Lee T Schaller, Jill R Cowan, Steve S Gonzales, Gina S Lowell, C W Andrews, David J Reynolds, Marty St Clair, Richard J Hazen, Rob G Ferris, Katrina L Creech, Grace B 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.Entities:
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Year: 2004 PMID： 14971897 DOI： 10.1021/jm030255y
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446