title: Synthesis, cytotoxicity and structure-activity relationships between ester and amide functionalities in novel acridine-based platinum(II) complexes.
abstract: In order to improve the pharmacological profile of the anticancer drug cisplatin, several new acridine-based tethered (ethane-1,2-diamine)platinum(II) complexes connected by a polymethylene chain were synthetized. Activity-structure relationship between amide or ester functionalities was explored by changing acridine-9-carboxamide into acridine-9-carboxylate chromophore. The in vitro cytotoxicity of these new complexes was assessed in human colic HCT 116, SW480 and HT-29 cancer cell lines. Series of complexes bearing the acridine-9-carboxylate chromophore displayed higher cytotoxic effect than acridine-9-carboxamide complexes, with gradual effect according to the size of the polymethylene linker.
authors.affiliation: INSERM UMR U866, Facultés de Médecine & Pharmacie, 7 boulevard Jeanne d'Arc, BP 89700, 21079 Dijon cedex, France.
authors.forename: Florence
authors.initials: F
authors.lastname: Bouyer
authors.forename: Johnny
authors.initials: J
authors.lastname: Moretto
authors.forename: David
authors.initials: D
authors.lastname: Pertuit
authors.forename: Anna
authors.initials: A
authors.lastname: Szollosi
authors.forename: Marie-Aleth
authors.initials: MA
authors.lastname: Lacaille-Dubois
authors.forename: Yves
authors.initials: Y
authors.lastname: Blache
authors.forename: Bruno
authors.initials: B
authors.lastname: Chauffert
authors.forename: Nicolas
authors.initials: N
authors.lastname: Desbois
mesh_terms: D000166:Acridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D003603:Cytotoxins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D010984:Platinum / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000166:Acridines; D000970:Antineoplastic Agents; D003603:Cytotoxins; D010984:Platinum