Transition metals have an important place within medicinal biochemistry. The discovery of the anticancer drug cisplatin decades ago sparked a new era of metal-based pharmaceuticals and, since this time, various metal complexes have been explored for anticancer and other medicinal applications. Due to the lack of specificity and detrimental side effects of platinum drugs which are heavily used in the chemotherapeutic regimens, however, scientists are striving to find alternatives. 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. 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. 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 [Cu(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 NMR techniques, electronic absorption spectroscopy, electrochemical measurements and elemental analysis. The cytotoxicity evaluations were assessed against HELA cancer cells and compared with that of cisplatin.

Cu(II) mixed-ligand polypyridyl complexes with 6-mercaptopurine: Synthesis, characterization and their cytotoxicity evaluations

253rd National Meeting (2017)

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