title: Synthesis and biological activity of benzamide DNA minor groove binders.
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.
authors.affiliation: Department of Chemistry, Shaheed Benazir Bhutto University, Sheringal, Dir (Upper), Khyber Pakhtunkhwa, Pakistan; School of Chemical Sciences, University of Auckland, 23 Symonds St, Auckland, New Zealand.
authors.forename: Gul Shahzada
authors.initials: GS
authors.lastname: Khan
authors.affiliation: School of Chemical Sciences, University of Auckland, 23 Symonds St, Auckland, New Zealand.
authors.forename: Lisa I
authors.initials: LI
authors.lastname: Pilkington
authors.affiliation: School of Chemical Sciences, University of Auckland, 23 Symonds St, Auckland, New Zealand. Electronic address: d.barker@auckland.ac.nz.
authors.forename: David
authors.initials: D
authors.lastname: Barker
mesh_terms: D000478:Alkylation; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004247:DNA / Q000737:chemistry / Q000378:metabolism*; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009691:Nucleic Acid Denaturation; D044366:Transition Temperature
chemical_list: D000970:Antineoplastic Agents; D001549:Benzamides; D004247:DNA
keywords: Anti-proliferative; Benzamides; DNA binding agents; DNA melting analysis; Minor groove binders