Cellular Uptake, Cytotoxicity, and Metabolic Profiling of Human Cancer Cells Treated with Ruthenium(II) Polypyridyl Complexes [Ru(bpy) 2 (NN)]Cl 2 with NN=bpy, phen, dpq, dppz, and dppn

A series of five ruthenium(II) polypyridyl complexes [Ru(bpy) 2 (NN)]Cl 2 was tested against human HT‐29 and MCF‐7 cancer cell lines. Cellular uptake efficiency and cytotoxicity were found to increase with the size of the aromatic surface area of the NN ligand. The most active compound carrying th...

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Bibliographic Details
Published in:ChemMedChem 2008-07, Vol.3 (7), p.1104-1109
Main Authors: Schatzschneider, Ulrich, Niesel, Johanna, Ott, Ingo, Gust, Ronald, Alborzinia, Hamed, Wölfl, Stefan
Format: Article
Language:English
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Summary:A series of five ruthenium(II) polypyridyl complexes [Ru(bpy) 2 (NN)]Cl 2 was tested against human HT‐29 and MCF‐7 cancer cell lines. Cellular uptake efficiency and cytotoxicity were found to increase with the size of the aromatic surface area of the NN ligand. The most active compound carrying the dppn ligand exhibits a low micromolar IC 50 value against both cell lines comparable to that of cisplatin under similar conditions. Continuous measurement of oxygen consumption, extracellular acidification rate, and impedance of the cell layer with a chip‐based sensor system upon exposure to the complexes showed only small changes for the first two parameters throughout the series. A significant and irreversible decrease in impedance was, however, found for the dppn compound. This suggests that its biological activity is related to modifications in cell morphology or cell–cell and cell–matrix contacts.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.200800039