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Abstract The reaction of gold reagents HAuCl 4 •3H 2 O, AuCl (tht), or cyclometalated gold (III) precursor, CNAuCl 2 with chiral ( (R, R) - (-) -2, 3-bis (t-butylmethylphosphino) quinoxaline) and non-chiral phosphine (1, 2-Bis (diphenylphosphino) ethane, dppe) ligands lead to distorted Au (I), (1, 2, 4, 5) and novel cyclometalated Au (III) complexes (3, 6). These gold compounds were characterized by multinuclear NMR, microanalysis, mass spectrometry, and X-ray crystallography. The inherent electrochemical properties of the gold complexes were also studied by cyclic voltammetry and theoretical insight of the complexes was gained by density functional theory and TD-DFT calculations. The complexes effectively kill cancer cells with IC 50 in the range of ~0. 10–2. 53 μΜ across K562, H460, and OVCAR8 cell lines. In addition, the retinal pigment epithelial cell line, RPE-Neo was used as a healthy cell line for comparison. Differential cellular uptake in cancer cells was observed for the compounds by measuring the intracellular accumulation of gold using ICP-OES. Furthermore, the compounds trigger early – late stage apoptosis through potential disruption of redox homeostasis. Complexes 1 and 3 induce predominant G1 cell cycle arrest. Results presented in this report suggest that stable gold-phosphine complexes with variable oxidation states hold promise in anticancer drug discovery and need further development.
Kim et al. (Mon,) studied this question.