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

  1. Author:
    Dash, C.
    Ahmadibeni, Y.
    Hanley, M. J.
    Pandhare, J.
    Gotte, M.
    Le Grice, S. F. J.
    Parang, K.

  2. Author Address

    [Dash, C; Pandhare, J] Meharry Med Coll, Ctr AIDS Hlth Dispar Res, Dept Biochem & Canc Biol, Nashville, TN 37208 USA [Ahmadibeni, Y] Columbus State Univ, Dept Chem, Columbus, GA 31907 USA [Ahmadibeni, Y; Hanley, MJ; Parang, K] Univ Rhode Isl, Dept Biomed & Pharmaceut Sci, Kingston, RI 02881 USA [Gotte, M] McGill Univ, Dept Microbiol & Immunol, Montreal, PQ H3A 2T5, Canada [Le Grice, SFJ] NCI, Resistance Mech Lab, HIV Drug Resistance Program, Frederick, MD 21702 USA;Dash, C (reprint author), Meharry Med Coll, Ctr AIDS Hlth Dispar Res, Dept Biochem & Canc Biol, Nashville, TN 37208 USA;kparang@uri.edu
    1. Year: 2011
    2. Date: Jun
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 21
    2. 12
    3. Pages: 3519-3522
  4. Type of Article: Article
  5. ISSN: 0960-894X
  1. 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 beta-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 beta-triphosphate (1) and AZT beta-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 10 nM, 10 and 100 mu M, respectively. (C) 2011 Elsevier Ltd. All rights reserved.

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External Sources

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  2. DOI: 10.1016/j.bmcl.2011.05.005
  3. View record in Web of Science®
  4. WOS: 000291145900003

Library Notes

  1. Fiscal Year: FY2010-2011
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