Rapid synthesis and anti-proliferative properties of polyazamacrocycle-based bi- and tetra-gold(I) phosphine dithiocarbamate complexes.
Fiche publication
Date publication
avril 2019
Journal
Chembiochem : a European journal of chemical biology
Auteurs
Membres identifiés du Cancéropôle Est :
Pr BETTAIEB Ali, Pr PAUL Catherine
Tous les auteurs :
Flores O, Velic D, Mabrouk N, Bettaieb A, Tomasoni C, Robert JM, Paul C, Goze C, Roussakis C, Bodio E
Lien Pubmed
Résumé
A family of bimetallic and of tetrametallic phosphine-gold(I)-dithiocarbamate complexes were synthesized starting from cyclam and dimethylcyclam polyazamacrocycles respectively, along with their monometallic chlorido-phosphine gold(I) precursors. Their antiproliferative properties were evaluated on two cancer cell lines (A549 and NSCLC-N6-L16). Most of the mono and bimetallic complexes displayed strong activities, and especially one bimetallic derivatives showed anti-proliferative properties in the low micromolar range. Insights in the structure activity relationships were given, along with determination of thioredoxin reductase inhibition potential, two-photon imaging of the fluorescent derivatives, and evaluation of gold uptake.
Mots clés
cancer, dithiocarbamate, gold complexes, gold phosphine, polymetallic complexes
Référence
Chembiochem. 2019 Apr 10;: