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Date publication

novembre 2012

Auteurs

Membres identifiés du Cancéropôle Est :
Dr BELLEMIN-LAPONNAZ Stéphane , Pr FOURNEL Sylvie


Tous les auteurs :
Chardon E, Puleo GL, Dahm G, Fournel S, Guichard G, Bellemin-Laponnaz S

Résumé

In the search for novel metal-based pharmaceuticals, ruthenium-catalysed 1,3-dipolar cycloaddition is used to functionalise a series of palladium and platinum N-heterocyclic carbene complexes. This strategy was applied to the conjugation of amino acid, polyethylene glycol and oestradiol derivatives with the aim of enhancing chemical diversity and introducing specific features (e.g., water solubility, cell targeting). Antiproliferative activities of the different complexes were assayed against several cancer cell lines (KB, MCF7, HCT116, PC3, SKOV3, OVCAR8, HL60) and healthy cell lines (MRC5, VERO, EPC), which established their efficiency. The ease of the structural derivatisation thus renders these complexes attractive metal-based systems for the development of selective targeted metal-hybrid anticancer drugs.

Référence

. 2012 Nov;77(11):1028-38.