Title of article
Structure-based design of TACE selective inhibitors: Manipulations in the S1′–S3′ pocket Original Research Article
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
12
From page
6170
To page
6181
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.
Keywords
TACE inhibitors , ?-Sulfone hydroxamates , MMP selectivity
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2007
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306002
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