Investigation of photo-activation on ruthenium(II)–arene complexes for the discovery of potential selective cytotoxic agents. (1st November 2019) - Basu, Uttara
Graphical abstract: Four Ru(II)–arene complexes which are stable in DMF were found to display significant anti-proliferative properties against HeLa cancer cell line. We could also demonstrate the possibility to further activate the different complexes by light irradiation, which results in an increase of the anti-proliferative properties to a factor up to 2.5. Abstract: Rational design of ruthenium complexes with optimized ligands is a promising approach to modulate their stability and antiproliferative effects in cancerous cells. The release of ligands from the coordination sphere of the ruthenium complexes can lead to the formation of biologically active Ru species that are able to exert cytotoxic effects. Herein, we have studied this approach on four ruthenium(II) complexes bearing (3, 5-cycloheptadienyl)diphenylphosphine or (cycloheptyl)diphenylphosphine and ethylbenzoate or p-cymene and an unusual bimetallic analogue. The stability of the complexes was investigated in DMF as well as DMEM/FBS using 1 H and 31 P{ 1 H} NMR spectroscopy. We studied the photo-cytotoxicities of the complexes in two cell lines – HeLa and RPE-1 – to understand their behavior and cytotoxicity upon ligand dissociation. All complexes showed moderate to high cytotoxicity in the two cell lines upon light irradiation.