Title of article
Design and synthesis of 3,3-piperidine hydroxamate analogs as selective TACE inhibitors
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
4333
To page
4337
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.
Keywords
inflammation , TACE , rheumatoid arthritis
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798420
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