1. Cytotoxicity of cis-platinum(II) cycloaliphatic amidine complexes: Ring size and solvent effects on the biological activity.
- Author
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Marzano C, Sbovata SM, Gandin V, Michelin RA, Venzo A, Bertani R, and Seraglia R
- Subjects
- Antineoplastic Agents chemical synthesis, Antineoplastic Agents chemistry, Cell Line, Tumor, Cisplatin chemistry, Humans, Inhibitory Concentration 50, Molecular Structure, Solutions, Amidines chemistry, Antineoplastic Agents toxicity, Cisplatin chemical synthesis, Cisplatin toxicity, Heterocyclic Compounds chemistry, Solvents chemistry
- Abstract
A series of new platinum(II) amidine derivatives of the type cis-[PtCl(2){Z-NHC(NHR)Me}(2)] (R=cyclopropyl, 1; cyclopentyl, 2; cyclohexyl, 3) were prepared in high yield by addition of the corresponding cyclic aliphatic amine RNH(2) to the coordinated acetonitrile ligands in cis-[PtCl(2)(NCMe)(2)]. The solution behaviour of 1-3 has been studied in DMSO, PEG 400 (polyethylene glycol) and PEG-DME 500 (polyethylene glycol dimethylether). The amidine complexes 1-3 were evaluated for their cytotoxic properties against a panel of human tumor cell lines containing examples of cervix (HeLa), breast (MCF7), lung (A549) and colon (HCT-15) cancer. Moreover, the amidine complexes were tested for their cytotoxicity against normal human fibroblasts (HFF-1). For comparison purposes, the cytotoxicity of cisplatin was examined under the same experimental conditions. The results obtained showed that PEG and PEG-DME behave as good solvents to carry out biological assays with platinum complexes which are water-insoluble and unstable in DMSO. Complexes 2 and 3 exhibited a biological activity comparable to that of cisplatin.
- Published
- 2009
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