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

Kergreis Angélique | Zendy; Lord Rianne M. | Zendy; Pike Sarah J. | Zendy

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

Author(s) -

Kergreis Angélique,

Lord Rianne M.,

Pike Sarah J.

Publication year - 2020

Publication title -

chemistry – a european journal

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.687

H-Index - 242

eISSN - 1521-3765

pISSN - 0947-6539

DOI - 10.1002/chem.202002517

Subject(s) - platinum , pyrazine , chemistry , ligand (biochemistry) , cytotoxicity , cisplatin , selectivity , stereochemistry , triphenylphosphine , butane , medicinal chemistry , receptor , biochemistry , biology , in vitro , chemotherapy , catalysis , genetics

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)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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