Potent P1' Biphenylmethyl Substituted Aggrecanase Inhibitors.

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 (IC50=1.5 nM), and showed excellent selectivity over MMP-1 and MMP-9, with moderate selectivity against MMP-2.