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Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1 |
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| 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 |
| Affiliation: | GlaxoSmithKline Inc., 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. joe.h.chan@gsk.com |
| 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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