Author/Authors :
Jeffrey S. Condon، نويسنده , , Diane Joseph-McCarthy، نويسنده , , Jeremy I. Levin، نويسنده , , Henry-Georges Lombart، نويسنده , , Frank E. Lovering، نويسنده , , LinHong Sun، نويسنده , , Weiheng Wang، نويسنده , , Weixin Xu، نويسنده , , Yuhua Zhang، نويسنده ,
Abstract :
By focusing on the P1 portion of the piperidine β-sulfone ligands we identified a motif that induces selectivity and resulted in a series of TACE inhibitors that demonstrated excellent in vitro potency against isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and 14.