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Thiophenolato-bridged dinuclear arene ruthenium complexes: a new family of highly cytotoxic anticancer agents
Auteur(s)
Gras, Michaël
Zava, Olivier
Dyson, Paul J.
Date de parution
2010
In
Dalton Transactions, Royal Society of Chemistry (RSC), 2010/39//10305-10313
Résumé
New cationic diruthenium complexes of the type [(arene)<sub>2</sub>Ru<sub>2</sub>(SPh)<sub>3</sub>]<sup>+ </sup>, arene being C<sub>6</sub>H<sub>6</sub>, <i>p</i>-<sup>i</sup>PrC<sub>6</sub>H<sub>4</sub>Me, C<sub>6</sub>Me<sub>6</sub>, C<sub>6</sub>H<sub>5</sub>R, where R = (CH<sub>2</sub>)<i>n</i>OC(O)C<sub>6</sub>H<sub>4</sub>-p-O(CH<sub>2</sub>)<sub>6</sub>CH<sub>3</sub> or (CH<sub>2</sub>)<i>n</i>OC(O)CH[double bond, length as m-dash]CHC<sub>6</sub>H<sub>4</sub>-p-OCH<sub>3</sub> and <i>n</i> = 2 or 4, are obtained from the reaction of the corresponding precursor [(arene)RuCl<sub>2</sub>]<sub>2</sub> and thiophenol and isolated as their chloride salts. The complexes have been fully characterised by spectroscopic methods and the solid state structure of [(C<sub>6</sub>H<sub>6</sub>)<sub>2</sub>Ru<sub>2</sub>(SPh)<sub>3</sub>]<sup>+</sup>, crystallised as the hexafluorophosphate salt, has been established by single crystal X-ray diffraction. The complexes are highly cytotoxic against human ovarian cancer cells (cell lines A2780 and A2780cisR), with the IC50 values being in the submicromolar range. In comparison the analogous trishydroxythiophenolato compounds [(arene)<sub>2</sub>Ru<sub>2</sub>(S-<i>p</i>-C<sub>6</sub>H<sub>4</sub>OH)<sub>3</sub>]Cl (IC50 values around 100 μM) are much less cytotoxic. Thus, it would appear that the increased antiproliferative effect of the arene ruthenium complexes is due to the presence of the phenyl or toluyl substituents at the three thiolato bridges.
Identifiants
Type de publication
journal article
