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Demonstrates increased cytotoxicity of dinuclear platinum complexes in cancerous cells, highlighting therapeutic potential.
A series of cyclometallated mono‐ and di‐nuclear platinum(II) complexes and the parent organic ligand, 2,6‐diphenylpyridine 1 (HC^N^CH), have been synthesized and characterized. This library of compounds includes [(C^N^C)Pt II ( L )] ( L =dimethylsulfoxide (DMSO) 2 and triphenylphosphine (PPh 3 ) 3 ) and [((C^N^C)Pt II ) 2 ( L‘ )] (where L‘ = N ‐heterocycles (pyrazine (pyr) 4 , 4,4‘‐bipyridine (4,4‘‐bipy) 5 or diphosphine (1,4‐bis(diphenylphosphino)butane (dppb) 6 ). Their cytotoxicity was assessed against four cancerous cell lines and one normal cell line, with results highlighting significantly increased antiproliferative activity for the dinuclear complexes ( 4 – 6 ), when compared to the mononucleated species ( 2 and 3 ). Complex 6 is the most promising candidate, displaying very high selectivity towards cancerous cells, with selectivity index (SI) values >29.5 (A2780) and >11.2 (A2780cisR), and outperforming cisplatin by >4‐fold and >18‐fold, respectively.
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Kergreis et al. (2020) studied this question.
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