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J Med Chem. 2003 Aug 28;46(18):3840-52.

Stereospecific synthesis of 5-substituted 2-bisarylthiocyclopentane carboxylic acids as specific matrix metalloproteinase inhibitors.

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1
Institut de Recherches Servier, 125 chemin de Ronde, 78290 Croissy sur Seine, France, and Technologie Servier, 25-27 rue E. Vignat, 45007 Orléans, France.

Abstract

The synthesis and structure-activity relationship (SAR) studies of a series of cyclopentane carboxylic acid matrix metalloproteinase (MMP) inhibitors are described. Potent and specific MMP-2, -3, -9, -13 inhibitors were obtained by regio- and stereoselective substitutions at positions 2 and 5 on the cyclopentane ring. Compounds 2a and 2e are active in the mouse B16-F10 metastasis model and display very good pharmacokinetic parameters.

PMID:
12930146
DOI:
10.1021/jm0307638
[Indexed for MEDLINE]

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