Organic complexes of ruthenium have become of great interest as potential antineoplastic drugs. Many of them have confirmed anticancer properties in vitro and in vivo. They are usually less toxic and more selective than platinum compounds and have different mechanism of action. To the date, two ruthenium complexes: NAMI-A and KP 1019 entered the first phase of clinical trials.

Two novel ruthenium(II) complexes with flavone ligands have been synthetised in our laboratory and named Ru-134 and Ru-138. We also tested their cytotoxic and proapoptotic activity in comparison to cisplatin. The properties were evaluated towards bladder cancer cells EJ and EJcisR (a subline approx. seven times more resistant to cisplatin than EJ cells).

Ru-134 is 12 times less cytotoxic towards EJ cells than cisplatin and 2.5 times less cytotoxic towards EJcisR cells than cisplatin. That may suggest that it can partly overcome cisplatin resistance. Ru-134 is also 3.5 times less cytotoxic than cisplatin to HeLa cells. Double staining assay shows that Ru-134 can induce apoptosis quicker than cisplatin in their IC₅₀ concentrations. Ru-138 is significantly more cytotoxic than Ru-134, it is only three times less cytotoxic than cisplatin towards EJ cells.

Our results and literature data encourage us to continue the research and to investigate the group of ruthenium compounds as potential anticancer agents.

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