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Combining [Arene–Ru] with Azocarboxamide to Generate a Complex with Cytotoxic Properties
Authors:Michael G Sommer  Petra Kureljak  Dr Damijana Urankar  Dr David Schweinfurth  Nikolina Stojanovi?  Dr Martina Bubrin  Dr Martin Gazvoda  Dr Maja Osmak  Prof?Dr Biprajit Sarkar  Prof?Dr Janez Ko?mrlj
Institution:1. Institut für Chemie und Biochemie, Anorganische Chemie, Freie Universit?t Berlin, Fabeckstra?e 34–36, 14195, Berlin (Germany);2. Division of Molecular Biology, Ru?er Bo?kovi? Institute, Bijeni?ka cesta 54, HR‐10000 Zagreb (Croatia);3. Faculty of Chemistry and Chemical Technology, University of Ljubljana, A?ker?eva 5, SI‐1000, Ljubljana (Slovenia)
Abstract:Azocarboxamide (azcH) has been combined for the first time with Ru–Cym] to generate metal complexes with N,N‐ and N,O‐coordination mode, (Cym)Ru(azc)Cl] and (Cym)Ru(azcH)Cl]+PF6]?. Geometric and electronic structures of the complexes are reported along with their in vitro activities against different tumour cell lines and preliminary results on solution chemistry. Compound (Cym)Ru(azc)Cl] exhibited remarkable cytotoxic properties. It was cell‐type specific and had comparable IC50 values towards both cancer cells and their drug‐resistant subline. A tenfold increase in the sensitivity towards (Cym)Ru(azc)Cl] was noted for the tumour cells with depleted intracellular glutathione (GSH) level, suggesting the essential role of GSH in cell response to this compound.
Keywords:antitumor agents  azocarboxamide  N  N ligands  N  O ligands  ruthenium
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