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Madurahydroxylactone derivatives as dual inhibitors of human immunodeficiency virus type 1 integrase and RNase H

  1. Author:
    March, C.
    Beutler, J. A.
    Wamiru, A.
    Budihas, S.
    Mollmann, U.
    Heinisch, L.
    Mellors, J. W.
    Le Grice, S. F.
    Pommier, Y.

  2. Author Address

    Marchand, Christophe, Pommier, Yves] NCI, Canc Res Ctr, Mol Pharmacol Lab, Bethesda, MD 20892 USA. [Beutler, John A.; Wamiru, Antony] NCI, Canc Res Ctr, Mol Targets Dev Program, Frederick, MD USA. [Wamiru, Antony] SAIC, Frederick, MD USA. [Budihas, Scott, Le Grice, Stuart F.] NCI, Canc Res Ctr, HIV Drug Resistance Program, Frederick, MD USA. [Moellmann, Ute] Hans Knoell Inst, Leibniz Inst Nat Prod Res & Infect Biol, Dept Mol & Appl Microbiol, Jena, Germany. [Heinisch, Lothar] Hans Knoell Inst, Leibniz Inst Nat Prod Res & Infect Biol, Dept Biomol Chem, Jena, Germany. [Mellors, John W.] Univ Pittsburgh, Med Ctr, Div Infect Dis, Pittsburgh, PA USA.
    1. Year: 2008
  2. Journal: Antimicrobial Agents and Chemotherapy
    1. 52
    2. 1
    3. Pages: 361-364
  4. Type of Article: Article
  1. Abstract:

    A series of 29 madurahydroxylactone derivatives was evaluated for dual inhibition of human immunodeficiency virus type 1 (HIV-1) integrase and RNase H. While most of the compounds exhibited similar potencies for both enzymes, two of the derivatives showed 10- to 100-fold-higher selectivity for each enzyme, suggesting that distinct pharmacophore models could be generated. This study exemplifies the common and divergent structural requirements for the inhibition of two structurally related HIV-1 enzymes and demonstrates the importance of systematically screening for both integrase and RNase H when developing novel inhibitors.

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External Sources

  1. PMID: 17967911

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