Issue 2, 2015
From the journal:

MedChemComm

Cytotoxic peptide conjugates of dinuclear areneruthenium trithiolato complexes†

Federico Giannini,‡a   Marco Bartoloni,‡a   Lydia E. H. Paul,a   Georg Süss-Fink,b   Jean-Louis Reymond*a  and  Julien Furrer*a  

* Corresponding authors

a Departement für Chemie und Biochemie, Universität Bern, CH-3012 Bern, Switzerland
E-mail: jean-louis.reymond@dcb.unibe.ch, julien.furrer@dcb.unibe.ch

b Institut de Chimie, Université de Neuchâtel, CH-2000 Neuchâtel, Switzerland

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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Article information

DOI
https://doi.org/10.1039/C4MD00433G
Article type
Concise Article
Submitted
26 Sep 2014
Accepted
11 Nov 2014
First published
12 Nov 2014

Med. Chem. Commun., 2015,6, 347-350

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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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