期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 11, 页码 2521-2524出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.04.002
关键词
Legumain; Cancer; Cyano warhead; Protease inhibitor
资金
- Northern Ireland Department of Education and Learning (DEL)
- Invest Northern Ireland
- Heather Clarke Breast Cancer Foundation
This Letter describes the further development and SAR exploration of a novel series of Legumain inhibitors. Based upon a previously identified Legumain inhibitor from our group, we explored the SAR of the carbamate phenyl ring system to probe the P3 pocket of the enzyme. This led to the identification of a sub-nanomolar inhibitor of Legumain. (C) 2014 Elsevier Ltd. All rights reserved.
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