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Synthesis and study of cytotoxic diruthenium trithiolatocomplexes of the type [(η6-p-MeC6H4­Pri)2Ru2(μ2-SR)3]+

(F. Giannini, J. Furrer)

Recently, we have synthesized series of new cationic dinuclear arene ruthenium complexes of general formula
[(η6-arene)2Ru2(μ2-SR)3]+ and [(η6-arene)2Ru2(μ2-SR1)2(μ2-SR2)]+ and found them to be highly cytotoxic towards human ovarian cancer cells, the IC50 values being mostly in the submicromolar range. Incubation with possible biological targets such as nucleotides, peptides and amino acids revealed interactions with only cysteine and glutathione, causing oxidation to cystine and oxidized glutathione (GSSG), respectively. Systematic studies suggest that the cytotoxic activity is influenced by the lipophilicity and the Hammett’s constants of the corresponding thiols, although a direct correlation between cytotoxicity, catalytic oxidation activity and redox potentials cannot be established.

 

 

 

 

 

 

 

Further Projects - Overview

 

Synthesis of cationic dinuclear arene ruthenium complexes as the chloride salts ... full size

 

Further Reading

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F. Giannini, G. Süss-Fink, J. Furrer
Inorg. Chem. 50, 10552-10554, 2011.

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F. Giannini, J. Furrer, A-F. Ibao, G. Süss-Fink,
B. Therrien, O. Zava, M. Baquie, P. Dyson,
P. Stepnicka
J. Biol. Inorg. Chem. 17, 951-960, 2012.

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F. Giannini, L. Paul, J. Furrer
Chimia 65, 775-780, 2012.

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F. Giannini, J. Furrer, G. Süss-Fink, C. Clavel,
P. Dyson, J. Organomet
Chem. 2013, in press.

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F. Giannini, L. Paul, J. Furrer, B. Therrien, 
G. Süss-Fink
New J. Chem. 2013, in press.