The field of medicinal inorganic chemistry was revolutionized after the serendipitous discovery of the antitumor drug cisplatin (cis-[Pt(NH3)2Cl2) by Rosenberg et al in 1965 followed by its approval by FDA in 1978 due to its remarkable antiproliferative properties. In spite of its remarkable success and high cure rates, new drugs with fewer severe side effects, reduced tumor resistance and different mechanisms of action are needed. In addition, the development of anticancer agents that are effective against many different tumors is imperative due to the alarming number of new cases of cancer diagnosed every year. Among the many early and late transition metal-based potential anticancer drugs, ruthenium (Ru) compounds, such as NAMI-A, KP1019, several organometallic and luminescent polypyridine Ru(II) compounds having displayed high anticancer activities against several cancer cell lines, have garnered a great deal of interest. Since most of the polypyridine Ru(II) antitumor compounds contain N-donor neutral ligands, we decided to introduce a β-diketone O^O- donor ligand of curcumin into the coordination sphere. We have synthesized two (2) new monocationic polypyridine Ru(II) complexes, [Ru(bpy)2(curc)]+ (1), [Ru(phen)2(curc)]+ (2), where curc = curcumin ((1E,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl -1,6-heptadiene-3,5-dione) which were characterized by NMR, ESI-MS, electronic absorption spectroscopy and single crystal X-ray diffraction. Their anticancer properties were assessed against OVCAR-8 ovarian cancer cells compared with that of cisplatin.

Cytotoxicity studies of ruthenium(II) polypyridine compounds with a β-diketone ligand

253rd National Meeting (2017)

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