Synthesis,characterization, DNA interaction studies and anticancer activity of platinum–clotrimazole complexes |
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Authors: | Maribel Navarro Angel Rubén Higuera-Padilla Miriam Arsenak Peter Taylor |
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Institution: | 1.Laboratorio de Química Bioinorgánica, Centro de Química,Instituto Venezolano de Investigaciones Científicas, (IVIC),Caracas,Venezuela;2.Laboratorio de Patología Celular y Molecular, Centro de Medicinal Experimental,Instituto Venezolano de Investigaciones Científicas, (IVIC),Caracas,Venezuela;3.Universidad de Carabobo,Valencia,Venezuela |
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Abstract: | New trans-platinum complexes of clotrimazole (CTZ) have been prepared and characterized. Their interaction with DNA and activity against
tumour cell lines were evaluated. Pt (CTZ)2I2] (1) was synthesized by the reaction of K2PtCl4, KI and CTZ, and Pt(CTZ)2Cl2] (2) by direct reaction of K2PtCl4 with CTZ. These complexes were characterized by a combination of elemental analysis, molar conductivity, UV–Vis, IR, and
NMR spectroscopy in one and two dimensions. DNA–platinum complex interactions were studied by spectroscopic, thermal denaturation
and viscosity titration measurements. Covalent interaction studies were also performed. From these results we suggest that
complexes 1 and 2 interact with the minor groove of DNA. Both complexes showed growth inhibitory effects on four out of the six tumour cells
lines with GI50 (50% growth inhibition) values in the 5–25 μM range, but there was no indication of cytotoxicity over the range of concentrations
tested. |
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