Author/Authors :
Adrian Huang، نويسنده , , Diane Joseph-McCarthy، نويسنده , , Frank Lovering، نويسنده , , LinHong Sun، نويسنده , , Weiheng Wang، نويسنده , , Weixin Xu، نويسنده , , Yi Zhu، نويسنده , , Junqing Cui، نويسنده , , Yuhua Zhang، نويسنده , , Jeremy I. Levin، نويسنده ,
Abstract :
A series of β-sulfonyl hydroxamate TACE inhibitors, bearing a butynylamino or a butynyloxy P1′ group, was designed and synthesized. Of the compounds investigated, 22 has excellent potency against isolated TACE enzyme, shows good selectivity over MMP-2 and MMP-13, and oral activity in an in vivo mouse model of TNF-α production.
