| Literature DB >> 20869872 |
Peter D Williams1, Donnette D Staas, Shankar Venkatraman, H Marie Loughran, Rowena D Ruzek, Theresa M Booth, Terry A Lyle, John S Wai, Joseph P Vacca, Bradley P Feuston, Linda T Ecto, Jessica A Flynn, Daniel J DiStefano, Daria J Hazuda, Carolyn M Bahnck, Amy L Himmelberger, Geetha Dornadula, Renee C Hrin, Kara A Stillmock, Marc V Witmer, Michael D Miller, Jay A Grobler.
Abstract
Optimization studies using an HIV RNase H active site inhibitor containing a 1-hydroxy-1,8-naphthyridin-2(1H)-one core identified 4-position substituents that provided several potent and selective inhibitors. The best compound was potent and selective in biochemical assays (IC(50)=0.045 μM, HIV RT RNase H; 13 μM, HIV RT-polymerase; 24 μM, HIV integrase) and showed antiviral efficacy in a single-cycle viral replication assay in P4-2 cells (IC(50)=0.19 μM) with a modest window with respect to cytotoxicity (CC(50)=3.3 μM).Entities:
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Year: 2010 PMID： 20869872 DOI： 10.1016/j.bmcl.2010.08.135
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823