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Elsevier, European Journal of Medicinal Chemistry, 11(46), p. 5456-5464, 2011

DOI: 10.1016/j.ejmech.2011.09.006

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Synthesis and characterization of novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes with higher cytotoxicity than cisplatin

Journal article published in 2011 by Hristo Varbanov, Seied M. Valiahdi, Anton A. Legin, Michael A. Jakupec ORCID, Alexander Roller, Markus Galanski, Bernhard K. Keppler
This paper is made freely available by the publisher.
This paper is made freely available by the publisher.

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Abstract

A series of six novel bis(carboxylato)dichloridobis(ethylamine)platinum(IV) complexes was synthesized and characterized in detail by elemental analysis, FT-IR, ESI-MS, HPLC, multinuclear ((1)H, (13)C, (15)N, (195)Pt) NMR spectroscopy and in one case by X-ray diffraction. Cytotoxic properties of the complexes were evaluated in four human tumor cell lines originating from ovarian carcinoma (CH1 and SK-OV-3), colon carcinoma (SW480) and non-small cell lung cancer (A549) by means of the MTT colorimetrical assay. In addition, their octanol/water partition coefficients (log P values) were determined. Remarkably the most active (and also most lipophilic) compounds, having 4-propyloxy-4-oxobutanoato and 4-(2-propyloxy)-4-oxobutanoato axial ligands, showed IC(50) values down to the low nanomolar range.