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Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors

  1. Author:
    Zhao, X. Z.
    Maddali, K.
    Metifiot, M.
    Smith, S. J.
    Vu, B. C.
    March, C.
    Hughes, S. H.
    Pommier, Y.
    Burke, T. R.

  2. Author Address

    [Zhao, XZ; Burke, TR] NCI, Biol Chem Lab, Mol Discovery Program, Ctr Canc Res,NIH, Frederick, MD 21702 USA [Maddali, K; Metifiot, M; Marchand, C; Pommier, Y] NCI, Mol Pharmacol Lab, Ctr Canc Res, NIH, Bethesda, MD 20892 USA [Smith, SJ; Vu, BC; Hughes, SH] NCI, HIV Drug Resistance Program, Ctr Canc Res, NIH, Frederick, MD 21702 USA;Zhao, XZ (reprint author), NCI, Biol Chem Lab, Mol Discovery Program, Ctr Canc Res,NIH, Frederick, MD 21702 USA;xuezhi.zhao@nih.gov tburke@helix.nih.gov
    1. Year: 2011
    2. Date: May
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 21
    2. 10
    3. Pages: 2986-2990
  4. Type of Article: Article
  5. ISSN: 0960-894X
  1. Abstract:

    New tricyclic HIV-1 integrase (IN) inhibitors were prepared that combined structural features of bicyclic pyrimidinones with recently disclosed 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones. This combination resulted in the introduction of a nitrogen into the aryl ring and the addition of a fused third ring to our previously described inhibitors. The resulting analogues showed low micromolar inhibitory potency in in vitro HIV-1 integrase assays, with good selectivity for strand transfer relative to 3'-processing. Published by Elsevier Ltd.

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External Sources

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  2. DOI: 10.1016/j.bmcl.2011.03.047
  3. View record in Web of Science®
  4. WOS: 000290024200041

Library Notes

  1. Fiscal Year: FY2010-2011
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