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Design and synthesis of photoactivatable aryl diketo acid-containing HIV-1 integrase inhibitors as potential affinity probes

  1. Author:
    Zhang, X. C.
    March, C.
    Pommier, Y.
    Burke, T. R.

  2. Author Address

    Burke, TR, NCI, Canc Res Ctr, Med Chem Lab, POB B,Bldg 376 Boyles St, Frederick, MD 21702 USA NCI, Canc Res Ctr, Med Chem Lab, Frederick, MD 21702 USA. NCI, Lab Mol, Ctr Canc Res, NIH, Bethesda, MD 20892 USA.
    1. Year: 2004
    2. Date: Mar 8
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 14
    2. 5
    3. Pages: 1205-1207
  4. Type of Article: Article
  1. Abstract:

    Aryl diketo acids (ADKs) represent an important new class of HIV-1 integrase (IN) inhibitors. In order to facilitate examination of the structural basis underlying IN.ADK interaction, biphenyl ketone and phenyl azide photophores were incorporated into ADK structures. Of particular note is the novel dual utilization of azide and phenyketone moieties for both enzyme recognition and for crosslinking. The resulting analogues maintained low micromolar inhibitory potency against IN in recombinant in vitro assays. These potential HIV-1 integrase photoaffinity labels may provide useful tools for studying enzyme interactions of the ADK inhibitor class. Published by Elsevier Ltd

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  2. DOI: 10.1016/j.bmcl.2003.12.064
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