| Affiliation: | 1. CNRS, Université Bourgogne Franche-Comté, ICMUB UMR6302, 9 avenue Alain Savary, 21000 Dijon, France;2. Université de Nantes, UFR Sciences Pharmaceutiques, Laboratoire IIciMed EA1155, Département de Cancérologie, 9 rue Bias, 44035 Nantes, France;3. EPHE, PSL Research University, Laboratoire d'Immunologie et Immunothérapie des Cancers, 60 Rue Mazarine, 75006 Paris, France
Université Bourgogne Franche-Comté, LIIC, EA7269, 7 Bd Jeanne d'Arc, 21000 Dijon, France |
| Abstract: | A family of bi- and tetrametallic gold(I) phosphine dithiocarbamate complexes were synthesized, starting from cyclam and dimethylcyclam polyazamacrocycles, respectively, along with their monometallic gold(I) chloridophosphine 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, in particular, one bimetallic derivative showed antiproliferative properties in the low micromolar range. Insights into the structure–activity relationships are given, along with determination of the thioredoxin reductase inhibition potential, two-photon imaging of the fluorescent derivatives, and evaluation of gold uptake. |
