Author/Authors :
Wenqing Yao، نويسنده , , Michael Chao، نويسنده , , Zelda R. Wasserman، نويسنده , , Ruiqin Liu، نويسنده , , Maryanne B. Covington، نويسنده , , Robert Newton، نويسنده , , David Christ، نويسنده , , Ruth R. Wexler، نويسنده , , Carl P. Decicco، نويسنده ,
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.