Arene-ruthenium(II) complexes containing 5-fluorouracil-1-methyl isonicotinate: Synthesis and characterization of their anticancer activity

To integrate the respective advantages exhibited by half-sandwich arene-Ru(II) fragments and 5-FU derivatives, a multifunctional ligand that links isonicotinic acid and 5-Fu (5-fluorouracil) through an ester bond for achieving the enhanced effect and an organoruthenium(II) complex containing this ligand were prepared and characterized by standard analytical techniques. The cytotoxicity of these organoruthenium(II) compounds containing 5-fluorouracil-1-methyl isonicotinate against BEL-7402 human cancer cells was moderately improved, which implies synergistic action of 5-Fu and the half-sandwich-structured arene-Ru(II). In addition, the organoruthenium(II) compounds containing isonicotinic acid and methyl isonicotinate are also discussed, and the crystal structure of [(η6-p-cymene)RuCl2(methyl isonicotinate)] (4) was determined; its piano-stool structure is analyzed in this paper.

A series of organoruthenium(II) complexes that contain isonicotinic acid derivatives were prepared, and the cytotoxicity of the first organoruthenium(II) compound containing 5-fluorouracil-1-methyl isonicotinate on the growth of BEL-7402 cells was found to be moderate, thereby showing synergistic action between the complex and the isonicotinic acid derivative.Figure optionsDownload as PowerPoint slideHighlights
► First 5-fluorouracil-1-methyl isonicotinate is combined with arene-Ru(II) fragments.
► Arene-ruthenium(II) complexes show moderate anticancer activity in vitro.
► One piano-stool crystal structure of arene-Ru(II) complex is discussed.