Identification and SAR exploration of a novel series of Legumain inhibitors

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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 languageEnglish
Pages (from-to)1546-1548
Number of pages3
JournalBioorganic & Medicinal Chemistry Letters
Volume29
Issue number12
Early online date29 Mar 2019
DOIs
Publication statusPublished - 15 Jun 2019

Bibliographical note

Crown Copyright © 2019. Published by Elsevier Ltd. All rights reserved.

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