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

Angélique Kergreis, Rianne M. Lord, Sarah J. Pike

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)
93 Downloads (Pure)

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.
Original languageEnglish
JournalChemistry: A European Journal
Early online date10 Jun 2020
DOIs
Publication statusE-pub ahead of print - 10 Jun 2020

Keywords

  • anticancer
  • bioinorganic chemistry
  • cyclometallated platinum(II)
  • multinuclear complexes
  • phosphine ligands

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