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Potent P1' biphenylmethyl substituted aggrecanase inhibitors
Wenqing Yao1, Michael Chao, Zelda R Wasserman
1Department of Chemistry, Bristol-Myers Squibb Pharma Company, Experimental Station, Wilmington, DE 19880-0500, USA. wenping.yao@dupontpharma.com
Bioorganic & Medicinal Chemistry Letters
|December 12, 2001
Abstract:
A series of cis-1(S)2(R)-amino-2-indanol based compounds with a biphenylmethyl group at the P1' position was found to be potent aggrecanase inhibitors. Both compounds 2j and 2n possessed very high aggrecanase affinity (IC(50)=1.5nM), and showed excellent selectivity over MMP-1 and MMP-9, with moderate selectivity against MMP-2.