Cytotoxic peptide conjugates of dinuclear arene ruthenium trithiolato complexes


Autoria(s): Giannini, Federico; Bartoloni, Marco; Paul, Lydia E. H.; Süss-Fink, Georg; Reymond, Jean-Louis; Furrer, Julien
Data(s)

2015

Resumo

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.

Formato

application/pdf

Identificador

http://boris.unibe.ch/61886/1/c4md00433g.pdf

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 <http://dx.doi.org/10.1039/c4md00433g>

doi:10.7892/boris.61886

info:doi:10.1039/c4md00433g

urn:issn:2040-2503

Idioma(s)

eng

Publicador

Royal Society of Chemistry

Relação

http://boris.unibe.ch/61886/

Direitos

info:eu-repo/semantics/restrictedAccess

Fonte

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 <http://dx.doi.org/10.1039/c4md00433g>

Palavras-Chave #570 Life sciences; biology #540 Chemistry
Tipo

info:eu-repo/semantics/article

info:eu-repo/semantics/publishedVersion

PeerReviewed