Abstract
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.
Original language | English |
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Pages (from-to) | 5642-5645 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 25 |
Issue number | 23 |
Early online date | 09 Oct 2015 |
DOIs | |
Publication status | Published - 01 Dec 2015 |