期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 6, 页码 1575-1580出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.02.024
关键词
ADAMTS-5 inhibitors
A series of N-substituted sulfonylamino-alkanecarboxylate ADAMTS-5 (Aggrecanase-2) inhibitors has been synthesized and the in vitro enzyme SAR is discussed. This report is the first example of carboxylate-based ADAMTS-5 inhibitors which show strong potency of IC50 < 0.1 mu M with excellent selectivity over MMP-1 and TACE. (C) 2009 Elsevier Ltd. All rights reserved.
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