title: Design and evaluation of biological activity of diazenecarboxamide-extended cisplatin and carboplatin analogues.
abstract: Construction of a library of structurally diverse diazenecarboxamide-extended cis-[Pt(2-picolyl-1,2,3-triazole)Cl2,] and cis-[Pt(propan-1,3-diamine)CBDCA] (CBDCA = 1,1 -cyclobutanedicarboxylate) complexes 1-4 is described. These compounds retain oxidative properties of parent diazenecarboxamides against glutathione as demonstrated by NMR spectroscopy and high resolution mass spectrometry experiments. Cytotoxic activity of 1-4 was investigated against human cervical carcinoma HeLa cells. Four library members were found to possess moderate cytotoxic activity. Some model compounds were also examined, returning [PtCl2L2] (L = 1-(2-picolyl)-4-phenyl-1H-1,2,3-triazole) as the most potent under this investigation with IC50 of 19.05 microM, comparable to that of cisplatin (IC50 = 16.3 microM).
authors.affiliation: Division of Molecular Biology, Ruder Bosković lnstitute, Zagreb, Croatia.
authors.forename: Nikolina
authors.initials: N
authors.lastname: Stojanovic
authors.forename: Damijana
authors.initials: D
authors.lastname: Urankar
authors.forename: Anamaria
authors.initials: A
authors.lastname: Brozović
authors.forename: Andreja
authors.initials: A
authors.lastname: Ambriović-Ristov
authors.forename: Maja
authors.initials: M
authors.lastname: Osmak
authors.forename: Janez
authors.initials: J
authors.lastname: Kosmrlj
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D016190:Carboplatin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D002853:Chromatography, Liquid; D002945:Cisplatin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D016190:Carboplatin; D002945:Cisplatin