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Issue 2, 2015
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Cytotoxic peptide conjugates of dinuclear areneruthenium trithiolato complexes

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Abstract

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.

Graphical abstract: Cytotoxic peptide conjugates of dinuclear arene ruthenium trithiolato complexes

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Supplementary files

Article information


Submitted
26 Sep 2014
Accepted
11 Nov 2014
First published
12 Nov 2014

Med. Chem. Commun., 2015,6, 347-350
Article type
Concise Article
Author version available

Cytotoxic peptide conjugates of dinuclear arene ruthenium trithiolato complexes

F. Giannini, M. Bartoloni, L. E. H. Paul, G. Süss-Fink, J. Reymond and J. Furrer, Med. Chem. Commun., 2015, 6, 347
DOI: 10.1039/C4MD00433G

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