Library of second-generation cycloruthenated compounds and evaluation of their biological properties as potential anticancer drugs: passing the nanomolar barrier.
Fiche publication
Date publication
septembre 2011
Auteurs
Membres identifiés du Cancéropôle Est :
Dr GAIDDON Christian
Tous les auteurs :
Fetzer L, Boff B, Ali M, Xiangjun M, Collin JP, Sirlin C, Gaiddon C, Pfeffer M
Lien Pubmed
Résumé
A library of 32 organoruthenium compounds has been synthesised. Known and novel C-N cyclometalated compounds as well as N-C-N and N-N-C pincer derivatives of this metal have been used in this purpose. Most of the compounds have been tested for their in vitro antitumoral behaviours, good to excellent activities have thus been found. Several of the newly synthesized compounds pass the symbolic barrier of the nanomolar range for their IC(50) indicating a critical improvement. The level of activity is tentatively correlated to physicochemical properties of the compounds such as their Ru(III/II) redox potential and their lipophilicity (log P).
Référence
Dalton Trans. 2011 Sep 21;40(35):8869-78