Tuning the in vitro cell cytotoxicity of dinuclear arene ruthenium trithiolato complexes: Influence of the arene ligand

Giannini, Federico; Geiser, Lennart; Paul, Lydia E.H.; Roderer, Thomas; Therrien, Bruno; Süss-Fink, Georg; Furrer, Julien (2015). Tuning the in vitro cell cytotoxicity of dinuclear arene ruthenium trithiolato complexes: Influence of the arene ligand. Journal of organometallic chemistry, 783, pp. 40-45. Elsevier 10.1016/j.jorganchem.2015.02.010

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A new series of cationic dinuclear arene ruthenium complexes bridged by three thiophenolato ligands, [(η6-arene)2Ru2(μ2-SR)3]+ with arene = indane, R = met: 1 (met = 4-methylphenyl); R = mco: 4 (mco = 4-methylcoumarin-7-yl); arene = biphenyl, R = met: 2; R = mco: 5; arene = 1,2,3,4-tetrahydronaphthalene, R = met: 3; R = mco: 6, have been prepared from the reaction of the neutral precursor [(η6-arene)Ru(μ2-Cl)Cl]2 and the corresponding thiophenol RSH. All cationic complexes have been isolated as chloride salts and fully characterized by spectroscopic and analytical methods. The molecular structure of 1, solved by X-ray structure analysis of a single crystal of the chloride salt, shows the two ruthenium atoms adopting a pseudo-octahedral geometry without metal–metal bond in accordance with the noble gas rule. All complexes are stable in H2O at 37 °C, but only 1 remains soluble in a 100 mM aqueous NaCl solution, while significant percentages (30–60 %) of 2–6 precipitate as chloride salts under these conditions. The 4-methylphenylthiolato complexes (R = met) are highly cytotoxic towards human ovarian cancer cells, the IC50 values being in the sub-micromolar range, while the 4-methylcoumarin-7-yl thiolato complexes (R = mco) are only slightly cytotoxic. Complexes 1 and 3 show the highest in vitro anticancer activity with IC50 values inferior to 0.06 μM for the A2780 cell line. The results demonstrate that the arene ligand is an important parameter that should be more systematically evaluated when designing new half-sandwich organometallic complexes.

Item Type:

Journal Article (Original Article)

Division/Institute:

08 Faculty of Science > Departement of Chemistry and Biochemistry
07 Faculty of Human Sciences > Institute of Psychology > Developmental Psychology
13 Central Units > General Secretariat > General Secretariat

UniBE Contributor:

Giannini, Federico; Roderer, Thomas and Furrer, Julien

Subjects:

500 Science > 570 Life sciences; biology
500 Science > 540 Chemistry
100 Philosophy > 150 Psychology

ISSN:

0022-328X

Publisher:

Elsevier

Language:

English

Submitter:

Julien Henri Lucien Furrer

Date Deposited:

11 Mar 2015 16:47

Last Modified:

14 Sep 2015 10:11

Publisher DOI:

10.1016/j.jorganchem.2015.02.010

BORIS DOI:

10.7892/boris.64312

URI:

https://boris.unibe.ch/id/eprint/64312

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