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Updated: Aug 5, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1
Joseph H Chan1, George A Freeman, Jeffrey H Tidwell
1GlaxoSmithKline 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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