Synthesis, structure and in vitro anticancer activity of ruthenium(II) and platinum(II) complexes with chiral aminophosphine ligands

(R)-[Ru(eta(6)-p-(MeC6H4Pr)-Pr-i)Cl-2{Ph2PNHCH(CH3)(C6H4-4-F)}] (1) and cis-(R,R)-[PtCl2{Ph2PNHCH(CH3)(C6H4-4-F)}(2)] (2) have been obtained by the reaction of the chiral aminophosphine (R)-Ph2PNHCH(CH3)(C6H4-4-F) with [{RuCl(mu-Cl)(eta(6)-p-(MeC6H4Pr)-Pr-i)}(2)] or [PtCl2(cod)] (cod = cycloocta-1,5-diene). Both complexes were characterized by physico-chemical and spectroscopic methods. Compound 1 was also characterized by X-ray crystallography. The antitumor potential of both compounds was investigated by using the crystal violet antiproliferation assay. Complexes 1 and 2 were found to inhibit the growth of three human cancer cell lines, whereby the Ru complex was considerably more potent than the Pt complex, with IC50 values between 1 and 3 and 12-15 mu M, respectively, but still less potent than cisplatin in the same three cell lines.

Automated summary

Two chiral aminophosphine metal complexes were synthesized and their potential antitumor activities were investigated. Experimental results showed that the ruthenium complex exhibited higher antitumor activity compared to the platinum complex, but still lower than cisplatin.