• Title of article

    Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity Original Research Article

  • Author/Authors

    Gwennaël LeDour، نويسنده , , Gautier Moroy، نويسنده , , Matthieu Rouffet، نويسنده , , Erika Bourguet، نويسنده , , Dominique Guillaume، نويسنده , , Martine Decarme، نويسنده , , Haquima ElMourabit، نويسنده , , Franck Augé، نويسنده , , Alain J.P. Alix، نويسنده , , Jean-Yves Laronze، نويسنده , , Georges Bellon، نويسنده , , William Hornebeck، نويسنده , , Janos Sapi، نويسنده ,

  • Issue Information
    روزنامه با شماره پیاپی سال 2008
  • Pages
    15
  • From page
    8745
  • To page
    8759
  • Abstract
    Hydrazide derivatives of Ilomastat, carrying either aryl groups or distinct alkyl and arylsulfonyl moieties were synthesized and evaluated for their MMP inhibitory activity. Potent and selective MMP-9 inhibition (IC50 = 3 nM) was observed for compound 3m (arylsulfonyl group: 4-(4-Br–C6H4)–C6H4–SO2–). Interaction with the S2 enzyme subsite is mainly responsible for the inhibitory properties of this derivative as confirmed by molecular docking computation.
  • Keywords
    Matrix metalloproteinase , Selective MMP-9 inhibition , Sulfonylhydrazide , Zinc-binding group , Ilomastat , Molecular modeling
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Serial Year
    2008
  • Journal title
    Bioorganic and Medicinal Chemistry
  • Record number

    1306891

    • Link To Document
    https://search.isc.ac/dl/search/defaultta.aspx?DTC=10&DC=1306891