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Design and evaluation of biological activity of diazenecarboxamide-extended cisplatin and carboplatin analogues

Construction of a library of structurally diverse diazenecarboxamide-extended cis-[Pt(2-picolyl-1, 2, 3-triazole)Cl-2] 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 mu M, comparable to that of cisplatin (IC50 = 16.3 mu M).

cisplatin; carboplatin; diazenecarboxamide; glutathione; anti-cancer activity

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