| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1376971 | Bioorganic & Medicinal Chemistry Letters | 2006 | 5 Pages |
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.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Kaapjoo Park, Alexis Aplasca, Mila T. Du, LinHong Sun, Yi Zhu, Yuhua Zhang, Jeremy I. Levin,