Synthesis and investigation of biological activities of goldN-heterocyclic carbene complex

In this thesis, 7 different Au-N-heterocyclic carbene (NHC) complexes were synthesized from Ag-NHC complexes via transmetallation. The synthesized NHC salts, Ag-NHC and Au-NHC complexes were characterized by widely used spectroscopic techniques. Anticancer activity, DNA binding, Xanthine Oxidase (XO) inhibitory activity studies of all Au-NHC complexes were evaluated to investigate the binding mechanism at the active site. The IC50value of Au-NHC complexes against human colorectal cancer (Caco-2) and breast cancer (MCF-7) celllines were determined by MTT method. IC50 values in the range of 5.2 ± 2 to 152.4 ± 1 for MCF-7 and 5.2 ± 1 to 152.7 ± 2 M for Caco-2, 3a, 3b, 3c, 3d and 3g were found to have beter anticancer activity than cisplatin. All Au-NHC complexes showed excellent antimicrobial activity against different bacteria and fungi. The complex belonging to group 3a showed the best antimicrobial activity. From the XO inhibitory activity assay results, all gold complexes showed remarkable inhibition activity against XO compared to the commonly used Standard allopurinol. The IC50 value for XO activity in the complex samples was determined between 0.409 ± 0.033 and 2.681 ± 0.091 μM. The 3d complex showed the lowest IC50 value of 0.409 ± 0.033 μM. It was determined that 3d was the most effective complex in antibacterial activity and 3e in antifungal activity. According to the results obtained from agarose gel images, the 3a complex bound to DNA more strongly than the other complexes and caused slow movement of the plasmid in super spiral form (I). Keywords: Au-NHC, Anticancer activity, DNA binding, Xanthine Oxidase