Luminescent Gold(I) Complexes of 1-Pyridyl-3-anthracenylchalcone Inducing Apoptosis in Colon Carcinoma Cells and Antivascular Effects.

The luminescent chalcone gold(I) conjugates [Au(PPh)(AN3)]PF() and [Au(SIMes)(AN3)]PF () (AN3 = ()-3-(9-anthracenyl)-1-(4-pyridyl)propenone; SIMes = ,'-dimesitylimidazolidin-2-ylidene; Mes = 2,4,6-trimethylphenyl)) were prepared and characterized; complex was also characterized by X-ray crystallography. In MTT assays against a panel of three human colon, a melanoma and a breast cancer cell lines both complexes were antiproliferative with low micromolar IC values. It is noteworthy that HCT116 colon carcinoma cells lacking functional p53 (a vital tumor suppressor) were more susceptible to them than the wildtype parent cell line. In flow cytometry analyses, the gold conjugates induced a significant arrest in G/M phase primarily. Complexes and quickly increased the production of reactive oxygen species (ROS) and induced mitochondrial membrane potential depolarization, higher ROS values being obtained after coadministration with enzymatic inhibitors. The free chalcone AN3 and its gold(I) complex conjugates located in the cell mitochondria according to confocal microscopy. In addition, complexes and showed antivascular effects on the chorioallantoic membrane (CAM) of fertilized specific-pathogen-free (SPF) chicken eggs.