Author/Authors :
Henry-Georges Lombart، نويسنده , , Eric Feyfant، نويسنده , , Diane Joseph-McCarthy، نويسنده , , Adrian Huang، نويسنده , , Frank Lovering، نويسنده , , LinHong Sun، نويسنده , , Yi Zhu، نويسنده , , Congmei Zeng، نويسنده , , Yuhua Zhang، نويسنده , , Jeremy Levin، نويسنده ,
Abstract :
Structure-based methods were used to design β-sulfone 3,3-piperidine hydroxamates as TACE inhibitors with the aim of improving selectivity for TACE versus MMP-13. Several compounds in this series were synthesized and evaluated in enzymatic and cell-based assays. These analogs exhibit excellent in vitro potency against isolated TACE enzyme and show good selectivity for TACE over the related metalloproteases MMP-2, -13, and -14.
