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Novel aryl diketo-containing inhibitors of HIV-1 integrase

  1. Author:
    Pais, G. C. G.
    Burke, T. R.
  2. Author Address

    NCI, Ctr Canc Res, Med Chem Lab, NIH, POB B,Bldg 376,Boyles St, Frederick, MD 21702 USA NCI, Ctr Canc Res, Med Chem Lab, NIH, Frederick, MD 21702 USA Burke TR NCI, Ctr Canc Res, Med Chem Lab, NIH, POB B,Bldg 376,Boyles St, Frederick, MD 21702 USA
    1. Year: 2002
  1. Journal: Drugs of the Future
    1. 27
    2. 11
    3. Pages: 1101-1111
  2. Type of Article: Review
  1. Abstract:

    HIV-1 integrase is a promising therapeutic target for the development of drugs to treat HIV infection. Aryl diketo-based analogs, disclosed independently by scientists from Merck and Shionogi pharmaceutical companies, are a unique class of compounds that exhibit potent integrase inhibition and display good antiviral effects in HIV-infected cells. The progress of Merck's L-870810 and Shionogi's S-1360 to phase 11 clinical trials has promised the inclusion of integrase inhibitors in "cocktail" combination therapies in the near future. This review presents a critical overview of research related to this new class of integrase inhibitors.

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