Fiche publication
Date publication
juillet 2014
Journal
ChemMedChem
Auteurs
Membres identifiés du Cancéropôle Est :
Pr DENAT Franck
Tous les auteurs :
Adriaenssens L, Liu Q, Chaux-Picquet F, Tasan S, Picquet M, Denat F, Le Gendre P, Marques F, Fernandes C, Mendes F, Gano L, Campello MP, Bodio E
Lien Pubmed
Résumé
A novel Ru(II) (arene) theranostic complex is presented. It is based on a 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid macrocycle bearing a triarylphosphine and can be tracked in vivo by using the γ emission of (153) Sm atoms. Notably, the heteroditopic ligand can be selectively metalated with ruthenium at the phosphorus atom despite the presence of other functionalities that are prone to metal coordination. Subsequent labeling with radionuclides such as (153) Sm can then be performed easily. The resulting heterobimetallic complex exhibits favorable solubility and stability properties in biologically relevant media. It also shows in vitro cytotoxicity in line with that expected for this type of metallodrug, and is nontoxic to the organism as a whole. As a proof of concept, initial studies in healthy mice were performed to obtain information about the uptake, biodistribution, and excretion of the radiolabeled complex.
Mots clés
Animals, Cell Line, Tumor, Cell Survival, drug effects, Coordination Complexes, chemical synthesis, Heterocyclic Compounds, 1-Ring, chemistry, Humans, Isotope Labeling, Mice, Phosphines, chemistry, Radiopharmaceuticals, chemical synthesis, Ruthenium, chemistry, Tissue Distribution, Water, chemistry
Référence
ChemMedChem. 2014 Jul;9(7):1567-73
