Deferasirox, an iron chelating ligand, has demonstrated antiproliferative activity due to its ability to decrease the bioavailability of the intracellular iron and thus inhibit iron-dependent biological pathways of the cell. Previous studies have shown that deferasirox produces an additive and synergistic effect when coupled with a metal. The titanium(IV) compound of deferasirox, (Ti(Def)<sub>2</sub>), has demonstrated potent cytotoxicity against a wide spectrum of cancer cell lines due to its potential of inhibiting the intracellular iron bioavailability via a transmetalation process. In this project, the main goal is to expand the toolset of the anticancer template by incorporating other metals ions, such as gold(III), whose biochemical properties can be manipulated for therapeutic function. In previous studies, Gold (I) and (III) complexes have demonstrated cytotoxic effect against cancer cells due to their capacity to disrupt the thioredoxin reductase system and disrupt the regulation of the reactive oxygen species (ROS). Therefore, the main objective of this project was to synthesize and characterize a gold(III) version of the deferasirox compound to examine whether this compound would demonstrate potent cytotoxicity against cancer cells. The synthesized compound was characterized by MALDI TOF/TOF, NMR spectroscopy, UV-Vis spectroscopy, and X-ray Powder Diffraction (XRD). The preliminary data obtained in this project suggest that a gold(III) deferasirox complex can be synthesized in a 1:2 metal:ligand stoichiometric ratio, possibly in a square planar modality.

Synthesis and characterization of a gold(III) deferasirox complex for an anticancer application

ACS Spring 2022

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