doi: 10.1021/jm030255y.
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1
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- PMID: 14971897
- DOI: 10.1021/jm030255y
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Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1
J Med Chem.
.
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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