Synthesis, characterisation and biological activity of the ruthenium(II) complexes of the N 4-tetradentate (N 4-T L), 1,6-di(2'-pyridyl)-2,5-dibenzyl-2,5-diazahexane (picenBz 2)

J Inorg Biochem. 2022 Jan;226:111629. doi: 10.1016/j.jinorgbio.2021.111629. Epub 2021 Oct 26.

Abstract

A series of complexes of the type rac-cis-β-[Ru(N4-TL)(N2-bidentates)]2+ (where N4-TL = 1,6-di(2'-pyridyl)-2,5-dibenzyl-2,5-diazahexane (picenBz2, N4-TL-2) and N2-bidentates = 1,10-phenanthroline (phen, Ru-2), dipyrido[3,2-d:2',3'-f]quinoxaline (dpq, Ru-3), 7,8-dimethyl-dipyrido[3,2-a:2',3'-c] phenazine (dppzMe2,Ru-4), 2-phenyl-1H-imidazo[4,5-f][1,10]phenanthroline (phenpyrBz, Ru-5), 2-(p-tolyl)-1H-imidazo[4,5-f][1,10]phenanthroline (phenpyrBzMe, Ru-6), 2-(4-nitrophenyl)-1H-imidazo[4,5-f][1,10]phenanthroline (phenpyrBzNO2,Ru-7), were synthesised and characterised and X-ray crystallography of Ru-5 obtained. The in vitro cytotoxicity assays revealed that Ru-6 was 5, 2 and 19-fold more potent than oxaliplatin, cisplatin, and carboplatin, respectively displaying an average GI50 value of ≈ 0.76 μM against a panel of 11 cancer cell lines.

Keywords: Cell growth inhibition; N(4)-tetradentate; Ruthenium.

Publication types

  • Research Support, Non-U.S. Gov't