Highly water soluble trithiolato-bridged dinuclear arene ruthenium complexes

• Synthesis of dinuclear arene ruthenium complexes bridged by thiolato ligands.
• The single-crystal X-ray structure analysis of three complexes is presented.
• The antiproliferative activity of the complexes has been evaluated in vitro.
• Two derivatives show an excellent selectivity for cancerous cells.

Water soluble arene-functionalised trithiolato-bridged ruthenium complexes of general formula [(η6-C6H5OCH2CH2OH)2Ru2(μ-SR)3]+, where R = C6H5 (1), C6H4-p-Me (2), C6H4-p-OMe (3), C6H4-p-Pri (4), C6H4-p-But (5), CH2C6H5 (6), CH2CH2C6H5 (7) and CH2C6H4-p-But (8), were prepared from the reaction of [(η6-C6H5OCH2CH2OH)2Ru2(μ-Cl)2Cl2] with the corresponding thiol, RSH. Complexes [1]Cl–[8]Cl were isolated in good yields as their chloride salts and they were fully characterised using spectroscopic and analytical techniques and the structures of [1]Cl, [3]Cl and [4]Cl were determined in the solid-state by single-crystal X-ray diffraction. The antiproliferative activity of [1]Cl–[8]Cl was evaluated against human ovarian cancer (A2780, A2780cisR) and non-cancerous (HEK293) cells with [4]Cl and [5]Cl being more active than cisplatin on the cancer cells and also more selective.

A series of trithiolato-bridged arene ruthenium complexes was synthesised and characterised. The antiproliferative activity of all complexes has been established. Two complexes showed an excellent selectivity for cancerous cells over a non-cancerous cell line, and both complexes were more cytotoxic than cisplatin on these cancerous cell lines.Figure optionsDownload as PowerPoint slide