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Bioorg Med Chem Lett. 2011 Jun 15;21(12):3519-22. doi: 10.1016/j.bmcl.2011.05.005. Epub 2011 May 8.

Inhibition of multi-drug resistant HIV-1 reverse transcriptase by nucleoside β-triphosphates.

Author information

  • 1Center for AIDS Health Disparities Research, Department of Biochemistry and Cancer Biology, Meharry Medical College, Nashville, TN 37208, USA.

Abstract

Despite the success of potent reverse transcriptase (RT) inhibitors against human immunodeficiency virus type 1 (HIV-1) in combination regimens, the development of drug resistant RTs constitutes a major hurdle for the long-term efficacy of current antiretroviral therapy. Nucleoside β-triphosphate analogs of adenosine and nucleoside reverse transcriptase inhibitors (NRTIs) (3'-azido-2',3'-dideoxythymidine (AZT), 3'-fluoro-2',3'-dideoxythymidine (FLT), and 2',3'-didehydro-2',3'-dideoxythymidine (d4T)) were synthesized and their inhibitory activities were evaluated against wild-type and multidrug resistant HIV-1 RTs. Adenosine β-triphosphate (1) and AZT β-triphosphate (2) completely inhibited the DNA polymerase activity of wild type, the NRTI multi resistant, and nonnucleoside RT inhibitors (NNRTI) resistant HIV-1 RT at 10nM, 10 and 100 μM, respectively.

Copyright © 2011 Elsevier Ltd. All rights reserved.

PMID:
21605974
[PubMed - indexed for MEDLINE]
PMCID:
PMC3114884
Free PMC Article

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