4.5 Article

Novel TNF-α converting enzyme (TACE) inhibitors as potential treatment for inflammatory diseases

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 24, 页码 7283-7287

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.10.081

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Hydantoin; TACE inhibitor; Rheumatoid arthritis

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Our research on hydantoin based TNF-alpha converting enzyme (TACE) inhibitors has led to an acetylene containing series that demonstrates sub-nanomolar potency (K-i) as well as excellent activity in human whole blood. These studies led to the discovery of highly potent TACE inhibitors with good DMPK profiles. Published by Elsevier Ltd.

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