Influence of Ligand and Nuclearity on the Cytotoxicity of Cyclometallated C^N^C Platinum(II) Complexes.

Chemistry : a European Journal
Angélique KergreisSarah J Pike

Abstract

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)PtII (L)] (L=dimethylsulfoxide (DMSO) 2 and triphenylphosphine (PPh3 ) 3) and [((C^N^C)PtII )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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Citations

Jan 27, 2021·Dalton Transactions : an International Journal of Inorganic Chemistry·Jonas F SchlagintweitFritz E Kühn

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Methods Mentioned

BETA
X‐ray
NMR
column chromatography

Software Mentioned

SHELXT
Graph Pad Prism
SHELXL
olex2

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