Abstract
Herein is reported the synthesis of two Au(III) complexes bearing the (R,R)-(–)-2,3-Bis(tert-butylmethylphosphino)quinoxaline (R,R-QuinoxP*) or (S,S)-(+)-2,3-Bis(tert-butylmethylphosphino)quinoxaline (S,S-QuinoxP*) ligands. By reacting two stoichiometric equivalents of HAuCl4.3H2O to one equivalent of the corresponding QuinoxP* ligand, (R,R)-(–)-2,3-Bis(tert-butylmethylphosphino)quinoxalinedichlorogold(III) tetrachloroaurates(III) (1) and (S,S)-(+)-2,3-Bis(tert-butylmethylphosphino)quinoxalinedichlorogold(III) tetrachloroaurates(III) (2) were formed, respectively, in moderate yields. The structure of (S,S)-(+)-2,3-Bis(tert-butylmethylphosphino)quinoxalinedichlorogold(III) tetrachloroaurates(III) (2) was further confirmed by X-ray crystallography. The antiproliferative activities of the two compounds were evaluated in a panel of cell lines and exhibited promising results comparable to auranofin and cisplatin with IC50 values between 1.08 and 4.83 µM. It is noteworthy that in comparison to other platinum and ruthenium enantiomeric complexes, the two enantiomers (1 and 2) do not exhibit different cytotoxic effects. The compounds exhibited stability in biologically relevant media over 48 h as well as inert reactivity to excess glutathione at 37 °C. These results demonstrate that the Au(III) atom, stabilized by the QuinoxP* ligand, can provide exciting compounds for novel anticancer drugs. These complexes provide a new scaffold to further develop a robust and diverse library of chiral phosphorus Au(III) complexes.
Highlights
The therapeutic application of metals is an ancient practice, dating back to the discovery of metals by man
Ligands, six cyclometalated gold complexes were synthesized with IC50 excellent antifungal activities in a panel of 21 Candida strains and 4 filamentous strains of Aspergillus the Fusarium micromolar range
R,R complex being more toxic than the S,S complex in we report the design and synthesis of two chiral Au(III) complexes bearing the chiral mammalian cells [39,40]
Summary
The therapeutic application of metals is an ancient practice, dating back to the discovery of metals by man. Ligands, six cyclometalated gold complexes were synthesized with IC50 excellent antifungal activities in a panel of 21 Candida strains and 4 filamentous strains of Aspergillus the Fusarium micromolar range These compounds were under physiological conditions with minimal sppinand spp [14,15]. Coordination of optically pure ethambutol ligand configuration and the ensuing platinum complexes possessing different biological activities [22]. The configuration of the FDA approved anticancer drug oxaliplatin is (1R,2R)platinum complexes possessing different biological activities [22]. This shows that the chirality of cyclohexane-1,2-diamine](ethanedioato-O,O’). Preliminary investigation into the biological activities of these two enantiomers shows no great difference in contrast to other enantiomeric platinum, ruthenium and osmium complexes
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