期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 12, 页码 1546-1548出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.03.019
关键词
Legumain; Small molecule inhibitor; SAR
资金
- Prostate Cancer UK through a Movember Project Grant [PG13-021]
- Invest Northern Ireland [RD0212980]
This letter describes the development of a series of potent and selective small molecule Legumain inhibitors suitable as chemical probes for in vitro experiments. Our previous research had identified a dipeptide inhibitor utilizing a semi-reversible cyano warhead that generated 2, a cell active inhibitor. This work explores an alternative P2-P3 linker and further SAR exploration of the P3 group which led to the identification of 16i, a highly potent inhibitor with excellent physiochemical properties.
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