| Literature DB >> 26522952 |
Kerry A Ness1, Sharon L Eddie1, Catherine A Higgins1, Amy Templeman1, Zenobia D'Costa1, Kishore K D Gaddale1, Samira Bouzzaoui1, Linda Jordan2, Dominic Janssen2, Timothy Harrison2, Frank Burkamp2, Andrew Young3, Roberta Burden3, Christopher J Scott3, Paul B Mullan1, Rich Williams4.
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.Entities:
Keywords: Cancer; Cellular active inhibitor; Cyano warhead; Legumain
Mesh：
Substances：
Year: 2015 PMID： 26522952 DOI： 10.1016/j.bmcl.2015.10.001
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823