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 > Department of Chemistry, Biochemistry and Pharmaceutical Sciences (DCBP) |
UniBE Contributor: |
Giannini, Federico, Bartoloni, Marco, Paul, Lydia, Reymond, Jean-Louis, 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: |
05 Dec 2022 14:39 |
Publisher DOI: |
10.1039/c4md00433g |
BORIS DOI: |
10.7892/boris.61886 |
URI: |
https://boris.unibe.ch/id/eprint/61886 |
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