4.5 Article

Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 18, Issue 1, Pages 241-246

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.10.093

Keywords

TACE inhibitor

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beta-Benzamido hydroxamic acids were discovered as potent TACE inhibitors. A computer model was constructed to help understanding the binding activities and guiding SAR study. SAR optimization led to the discovery of compound 30 which met all in vitro and in vivo criteria for the program and was selected for further evaluation. (C) 2007 Elsevier Ltd. All rights reserved.

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