Identification and SAR exploration of a novel series of Legumain inhibitors

Sharon L Eddie; Aaron Gregson; Emma Graham; Stephanie Burton; Timothy Harrison; Roberta Burden; Christopher J Scott; Paul B Mullan; Rich Williams

doi:10.1016/j.bmcl.2019.03.019

Identification and SAR exploration of a novel series of Legumain inhibitors

Sharon L Eddie, Aaron Gregson, Emma Graham, Stephanie Burton, Timothy Harrison, Roberta Burden, Christopher J Scott, Paul B Mullan, Rich Williams

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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.

Original language	English
Pages (from-to)	1546-1548
Number of pages	3
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	29
Issue number	12
Early online date	29 Mar 2019
DOIs	https://doi.org/10.1016/j.bmcl.2019.03.019
Publication status	Published - 15 Jun 2019

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AU - Graham, Emma

AU - Burton, Stephanie

AU - Harrison, Timothy

AU - Burden, Roberta

AU - Scott, Christopher J

AU - Mullan, Paul B

AU - Williams, Rich

PY - 2019/6/15

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AB - 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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JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

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Identification and SAR exploration of a novel series of Legumain inhibitors

Abstract

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