Synthesis and biological activity of benzamide DNA minor groove binders. Issue 3 (1st February 2016)

• Record Type: Journal Article
• Authors: Khan, Gul Shahzada; Pilkington, Lisa I.; Barker, David
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 3(2016)
• Page Start: 804
• Page End: 808
• Publication Date: 2016-02-01
• Subjects: DNA binding agents -- Minor groove binders -- Benzamides -- Anti-proliferative -- DNA melting analysis; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.12.090
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: A range of di- and triaryl benzamides were synthesised to investigate the effect of the presence and nature of a polar sidechain, bonding and substitution patterns and functionalisation of benzylic substituents. These compounds were tested for their antiproliferative activity as well as their DNA binding activity. The most active compounds in all assays were unsymmetrical triaryl benzamides with a bulky or alkylating benzylic substituent and a polar amino sidechain.