Cancer is the leading cause of death worldwide in developed countries and the second leading cause of death in developing countries following heart disease [1]. The serendipitous discovery of cisplatin [cis-[Pt(NH3)2Cl2] by Rosenberg et al sparked a new era of metal-based pharmaceuticals and various metal complexes have been explored for anticancer and other medicinal applications. Advances in coordination chemistry are crucial for improving the design of compounds to reduce toxic side effects and understand their mechanisms of action. However, the effectiveness of metal-based anticancer compounds is directly influenced by their coordination environment, specifically the ligands to which they are bound. The nature of the ligands can affect the anticancer activity of metal complexes as well as play pivotal roles in triggering other mechanisms which lead to cancer cell death [2]. Coordinatively saturated and kinetically inert coordination compounds have also been studied in cancer drug research. The structure of this class of molecules departs from the paradigm of using the inherent reactivity of the transition metal to exert a therapeutic effect by DNA binding, because there are no labile positions at the metal center in these compounds. Numerous examples of polypyridyl complexes that display promising anticancer properties have been reported [3,4]. In this study novel compounds were synthesized by the introduction of an anticancer drug as ligand into the coordination sphere to form mixed ligand metal complexes. The synthesis of new complexes of the type [Ru(N^N)2(6MP)][PF6] where N^N = 2,2-bipyridine (bpy, 1), 1,10-phenanthroline (phen, 2) and dipyrido[3,2-d:2’,3’-f]quinoxaline (dpq, 3) while 6MP = 6-mercaptopurine (3,7-dihydropurine-6-thione), have been synthesized and characterized by X-ray crystallography, NMR techniques, electronic absorption spectroscopy, electrochemical measurements and elemental analysis. The cytotoxicity evaluation was assessed against HeLa and OVCAR-8 cancer cells and compared with that of cisplatin.

Ruthenium polypyridyl complexes with mercaptopurine: Synthesis, characterization and cytotoxicity evaluation

256th National Meeting (2018)

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