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Cytotoxic peptide conjugates of dinuclear arene ruthenium trithiolato complexes

Type of publication Peer-reviewed
Publikationsform Original article (peer-reviewed)
Author Giannini Federico, Bartoloni Marco, Paul Lydia E. H., Süss-Fink Georg, Reymond Jean-Louis, Furrer Julien,
Project Exploring Peptide Topologies in Search for New Drugs
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Original article (peer-reviewed)

Journal MedChemCom
Volume (Issue) 2015(6)
Page(s) 347 - 350
Title of proceedings MedChemCom
DOI 10.1039/c4md00433g


In order to improve the water-solubility of dinuclear thiolato-bridged arene ruthenium complexes, a new series was synthesized by conjugating octaarginine, octalysine, and cyclo[Lys-Arg-Gly-Asp-D-Phe] using chloroacetyl thioether (ClAc) ligation, resulting in cytotoxic conjugates against A2780 human ovarian cancer cells (IC50 = 2–8 μM) and against the cisplatin resistant line A2780cisR (IC50 = 7–15 μM). These metal complexes represent, to the best of our knowledge, the most cytotoxic ruthenium bioconjugates reported so far.