Author/Authors :
Robert J. Cherney، نويسنده , , Carl P. Decicco، نويسنده , , David J. Nelson، نويسنده , , Li Wang، نويسنده , , Dayton T. Meyer، نويسنده , , Karl D. Hardman، نويسنده , , Robert A. Copeland، نويسنده , , Elizabeth C. Arner، نويسنده ,
Abstract :
Several carboxylate derivatives with variation at the P1′ residue were synthesized and evaluated as stromelysin (MMP-3) inhibitors. Compounds containing a biphenyl moiety at P1′ were found to be potent inhibitors of MMP-3. An X-ray crystal structure of the most potent compound, carboxylate 19, revealed an important interaction between the inhibitorʹs biphenyl and histidine 224 in the S1′ pocket of MMP-3.