期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 10, 页码 2699-2704出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.02.015
关键词
TACE inhibitors; metazincin; metalloprotease; sheddase; tumor necrosis factor; antiinflammatory; hydroxamic acid
A novel series of achiral TNF-alpha converting enzyme (TACE) inhibitors has been discovered. These compounds exhibited activities from 0.35 to 11 nM in a porcine TACE assay and inhibited TNF-alpha production in an LPS-stimulated whole blood assay with an IC50 value of 23 nM for the most potent one. They also have excellent selectivities over related metalloproteases including aggrecanases. (C) 2006 Elsevier Ltd. All rights reserved.
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