期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 23, 页码 5642-5645出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.10.001
关键词
Legumain; Cancer; Cyano warhead; Cellular active inhibitor
资金
- Invest Northern Ireland [RD0212980]
- Heather Clarke Memorial Breast Cancer fund, Prostate Cancer UK [PG13-021]
This Letter describes the continued SAR exploration of small molecule Legumain inhibitors with the aim of developing a potent and selective in vitro tool compound. Work continued in this Letter explores the use of alternative P2-P3 linker units and the P3 group SAR which led to the identification of 10t, a potent, selective and cellularly active Legumain inhibitor. We also demonstrate that 10t has activity in both cancer cell viability and colony formation assays. (C) 2015 Elsevier Ltd. All rights reserved.
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