Self-Assembly of Discrete Ru Molecular Cages and Their in Vitro Anticancer Activity.

Four new octanuclear Ru(II) cages (OC-1-OC-4) were synthesized from dinuclear p-cymene ruthenium(II) acceptors Ru(μ-η-CO)(CHOH)(η-p-cymene) (A), Ru(μ-η-CHO)(CHOH)(η-p-cymene) (A), Ru(dhnq)(HO)(η-p-cymene) (A), and Ru(dhtq)(HO)(η-p-cymene) (A) separately with a tetradentate pyridyl ligand (L) in methanol using coordination-driven self-assembly [L= N,N,N',N'-tetra(pyridin-4-yl)benzene-1,4-diamine]. The octanuclear cages are fully characterized by various spectroscopic techniques including single-crystal X-ray diffraction analysis of OC-4. The self-assembled cages show strong in vitro anticancer activity against human lung adenocarcinoma A549 and human cervical cancer HeLa cell lines as observed from the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Of all the octanuclear cages, OC-3 exhibits remarkable anticancer activity against both cancer cell lines and is more active than that reported for cisplatin. The excellent anticancer activity of OC-3 and OC-4 highlights the importance of the synergistic effects of the spacer component of the dinuclear p-cymene Ru(II) acceptor clips.