Identification and SAR exploration of a novel series of Legumain inhibitors.
Basic Information
ID: ALA4340539
Journal: Bioorg Med Chem Lett
Title: Identification and SAR exploration of a novel series of Legumain inhibitors.
Authors: Eddie SL, Gregson A, Graham E, Burton S, Harrison T, Burden R, Scott CJ, Mullan PB, Williams R.
Abstract: 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.
CiteXplore: 31005445
DOI: 10.1016/j.bmcl.2019.03.019
Patent ID: ┄