Syntheses of ruthenium(II)-4,4′-biimidazole complexes and their potential anti-tumour activity

Synthesis and characterization of the RuII complexes, [Ru(N−N)3][CF3SO3]2, where N−N is 4,4′-biimidazole (complex 1a) or 2,2′-dimethyl-4,4′-biimidazole (1b), and the dimethylsulfoxide complexes RuCl2(DMSO)2(N−N) are reported. The air-stable, water-soluble complexes were characterized by elemental analysis, 1H NMR and IR spectroscopies, mass spectrometry, and solution conductivity. Evidence is presented also for the existence of the diruthenium complexes Ru2Cl4(DMSO)4(N−N), but there are insufficient data for elucidation of their structure. The complexes (and cisplatin) were tested against human breast-cancer cells (MDA-MB-435S) using an in vitro MTT assay, a colorimetric determination of cell viability: 1a and 1b exhibit the lowest IC50 values of 18 ± 5 and 36 ± 5 µmol/L, respectively, with cisplatin exhibiting an IC50 value of 35 ± 5 µmol/L. Isolation of DNA from cells treated with a solution of the Ru species showed no evidence of DNA-binding to the metal, although examination of the cells indicated that Ru was being taken up into the cells.