Add time:07/16/2019         Source:sciencedirect.com

The synthesis, structural characterization and in vitro biological evaluation of two 2-(4′-aminophenyl)benzothiazole based ligands and their corresponding Pd(II) and Pt(II) complexes is reported. Their design was based on the selective anticancer action of phenylbenzothiazole in conjunction with the cytotoxicity of the metallic center, aiming at targeted and synergistic effectiveness of the complexes as anticancer agents. All compounds were fully characterized with IR, NMR and MS analysis and their binding to CT-DNA was investigated by UV–Vis spectroscopy, fluorescence, circular dichroism, viscometry, and thermal denaturation. The data indicate that both ligands interact with CT-DNA via a combined mode of action involving both groove binding and non-classical intercalation, while in the case of the complexes covalent bond formation takes place as well. The in vitro cytotoxicity and cell uptake studies in human breast carcinoma cell line (MCF-7 and MDA-MB-231) as well as in healthy human skin fibroblasts (DSF) show uptake of the intact complexes by cancer cells and increased activity against cancer cell lines.

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