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Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity |
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| Authors: | Ledour Gwennaël Moroy Gautier Rouffet Matthieu Bourguet Erika Guillaume Dominique Decarme Martine Elmourabit Haquima Augé Franck Alix Alain J P Laronze Jean-Yves Bellon Georges Hornebeck William Sapi Janos |
| Institution: | Université de Reims-Champagne-Ardenne, CNRS UMR 6229, Institut de Chimie Moléculaire de Reims, Faculté de Pharmacie, IFR53 Biomolécules, 51 rue de Cognacq-Jay, 51096 Reims Cedex, France. |
| 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 (IC(50)=3 nM) was observed for compound 3m (arylsulfonyl group: 4-(4-Br-C6H4)-C6H4-SO(2)-). Interaction with the S2 enzyme subsite is mainly responsible for the inhibitory properties of this derivative as confirmed by molecular docking computation. |
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