Combining [arene-Ru] with azocarboxamide to generate a complex with cytotoxic properties.
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.
Institut für Chemie und Biochemie, Anorganische Chemie, Freie Universität Berlin, Fabeckstraße 34-36, 14195, Berlin (Germany).
Michael G
MG
Sommer
Petra
P
Kureljak
Damijana
D
Urankar
David
D
Schweinfurth
Nikolina
N
Stojanović
Martina
M
Bubrin
Martin
M
Gazvoda
Maja
M
Osmak
Biprajit
B
Sarkar
Janez
J
Košmrlj
D000970:Antineoplastic Agents / Q000737:chemistry* / Q000633:toxicity; D001372:Aza Compounds / Q000737:chemistry*; D045744:Cell Line, Tumor; D056831:Coordination Complexes / Q000737:chemistry* / Q000633:toxicity; D018360:Crystallography, X-Ray; D005978:Glutathione / Q000737:chemistry*; D006801:Humans; D008958:Models, Molecular; D012428:Ruthenium / Q000737:chemistry*
D000970:Antineoplastic Agents; D001372:Aza Compounds; D056831:Coordination Complexes; D012428:Ruthenium; D005978:Glutathione
N,N ligands; N,O ligands; antitumor agents; azocarboxamide; ruthenium