Development of a potent and selective cell penetrant Legumain inhibitor

Kerry A. Ness, Sharon L Eddie, Catherine A Higgins, Amy Templeman, Zenobia D'Costa, Kishore K.D. Gaddale, Samira Bouzzaoui, Linda Jordan, Dominic Janssen, Timothy Harrison, Frank Burkamp, Andrew Young, Roberta Burden, Christopher J Scott, Paul B Mullan, Rich Williams

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6 Citations (Scopus)

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 languageEnglish
Pages (from-to)5642-5645
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number23
Early online date09 Oct 2015
DOIs
Publication statusPublished - 01 Dec 2015

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