Flat SAR of P3-methylsulphonamide based small molecule legumain inhibitors. Issue 2 (15th January 2016)

• Record Type: Journal Article
• Authors: Ness, Kerry Anne; Eddie, Sharon L.; Burton, Stephanie; Harrison, Timothy; Mullan, Paul; Williams, Rich
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 2(2016)
• Page Start: 413
• Page End: 416
• Publication Date: 2016-01-15
• Subjects: Legumain -- Cancer -- SAR -- Small molecule protease inhibitor; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.11.101
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: This letter describes the design, development and SAR exploration of a novel series of small legumain inhibitors. The SAR of a new small molecule legumain inhibitor chemotype was explored and found to have improved physiochemical properties compared to previously developed inhibitors within our group. However, further development of this series was found to be limited as the SAR was observed to be relatively flat.