Document Report Card

Basic Information

ID: ALA1135085

Journal: Bioorg Med Chem Lett

Title: Potent P1' biphenylmethyl substituted aggrecanase inhibitors.

Authors: Yao W, Chao M, Wasserman ZR, Liu RQ, Covington MB, Newton R, Christ D, Wexler RR, Decicco CP.

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.

CiteXplore: 11738583

DOI: 10.1016/s0960-894x(01)00704-1