Title of article
Design and synthesis of butynyloxyphenyl β-sulfone piperidine hydroxamates as TACE inhibitors
Author/Authors
Kaapjoo Park، نويسنده , , Alexis Aplasca، نويسنده , , Mila T. Du، نويسنده , , LinHong Sun، نويسنده , , Yi Zhu، نويسنده , , Yuhua Zhang، نويسنده , , Jeremy I. Levin، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
3927
To page
3931
Abstract
A series of butynyloxyphenyl β-sulfone piperidine hydroxamate TACE inhibitors was designed and synthesized. The resulting structure–activity relationship and MMP selectivity of the series were examined. Of the compounds investigated, 17s has excellent in vitro potency against isolated TACE enzyme, shows good selectivity over MMP-1, -2, -7, -8, -9, -13, and -14, and oral activity in an in vivo mouse model of TNF-α production.
Keywords
MMP selectivity , TACE inhibitors , structure–activity relationship , ?-Sulfone piperidine hydroxamates
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797106
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