Cytotoxic peptide conjugates of dinuclear arene ruthenium trithiolato complexes

Giannini, Federico; Bartoloni, Marco; Paul, Lydia E. H.; Süss-Fink, Georg; Reymond, Jean-Louis; Furrer, Julien (2015). Cytotoxic peptide conjugates of dinuclear arene ruthenium trithiolato complexes. Medicinal chemistry communications - MedChemComm, 6(2), pp. 347-350. Royal Society of Chemistry 10.1039/c4md00433g

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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.

Item Type:

Journal Article (Original Article)

Division/Institute:

08 Faculty of Science > Departement of Chemistry and Biochemistry

UniBE Contributor:

Giannini, Federico; Bartoloni, Marco; Paul, Lydia; Reymond, Jean-Louis and Furrer, Julien

Subjects:

500 Science > 570 Life sciences; biology
500 Science > 540 Chemistry

ISSN:

2040-2503

Publisher:

Royal Society of Chemistry

Language:

English

Submitter:

Julien Henri Lucien Furrer

Date Deposited:

26 Jan 2015 15:37

Last Modified:

15 Dec 2015 12:42

Publisher DOI:

10.1039/c4md00433g

BORIS DOI:

10.7892/boris.61886

URI:

https://boris.unibe.ch/id/eprint/61886

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