Water-Soluble Co(III) Complexes of Substituted Phenanthrolines with Cell Selective Anticancer Activity

Jagadeesan, S. and Balasubramanian, V. and Baumann, P. and Neuburger, M. and Haeussinger, D. and Palivan, C. G.. (2013) Water-Soluble Co(III) Complexes of Substituted Phenanthrolines with Cell Selective Anticancer Activity. Inorganic Chemistry, 52 (21). pp. 12535-12544.

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Official URL: http://edoc.unibas.ch/dok/A6212303

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Transition metal complexes with substituted phenanthrolines as ligands represent potential anticancer products without the drawbacks of platinum complexes that are currently marketed. Here, we report the synthesis and cell selective anticancer activity of five new water-soluble Co(III) complexes with methyl substituted phenanthroline ligands. The complexes were characterized by elemental analysis, NMR. FAB-mass spectrometry, FTIR, electronic spectroscopy, and single crystal X-ray diffraction. Possible interaction of these complexes with DNA was assessed by a combination of circular dichroism, UV-vis spectroscopy titration, and ethidium bromide displacement assay, and the results indicated that DNA interaction is weak for these complexes. Cellular uptake and cytotoxicity of complexes at low concentrations were assessed by flow cytometry on PC-3 cells, while their effect on intracellular mitochondrial function was measured by MTS assay on HeLa and PC-3 cell lines. These complexes showed selective cytotoxicity with a significantly higher effect on intracellular mitochondrial function in PC-3 cells than in He La cells. At low concentrations, complex 2 had the highest cytotoxic effect on PC-3 cells, inducing around 38% cell death, and the correlation of cytotoxicity of these complexes to their hydrophobicity indicates that an appropriate value of the hydrophobicity is essential for high antitumor activity.
Faculties and Departments:05 Faculty of Science > Departement Chemie > Former Organization Units Chemistry > Makromolekulare Chemie (Meier)
UniBasel Contributors:Palivan, Cornelia G and Häussinger, Daniel
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:American Chemical Society
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:04 Jun 2018 11:37
Deposited On:31 Jan 2014 09:50

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