2. Academic Validation
  3. Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1

Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1

  • J Med Chem. 2004 Feb 26;47(5):1175-82. doi: 10.1021/jm030255y.
Joseph H Chan 1,  George A Freeman,  Jeffrey H Tidwell,  Karen R Romines,  Lee T Schaller,  Jill R Cowan,  Steve S Gonzales,  Gina S Lowell,  C W Andrews 3rd,  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
Affiliations

Affiliation

  • 1 GlaxoSmithKline Inc., 5 Moore Drive, Research Triangle Park, North Carolina 27709, USA. [email protected]
PMID: 14971897 DOI: 10.1021/jm030255y
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.

Figures