In this work, gold(III) complexes stabilized by the Quinox P* ligand is reported. By reacting (R,R)-(–)-2,3-Bis(tert-butylmethylphosphino)quinoxaline (R,R-QuinoxP*) or (S,S)-(+)-2,3-Bis(tert-butylmethylphosphino)quinoxaline (S,S-QuinoxP*) with two stoichiometric equivalents of HAuCl4●3H2O, (R,R)-(–)-2,3-Bis(tert-butylmethylphosphino)quinoxalinedichlorogold(III) tetrachloroaurates(III) and (S,S)-(+)-2,3-Bis(tert-butylmethylphosphino)quinoxalinedichlorogold(III) tetrachloroaurates(III) were synthesized in average yields. (S,S)-(+)-2,3-Bis(tert-butylmethylphosphino)quinoxalinedichlorogold(III) tetrachloroaurates(III) crystallizes as a monocationic complex in a triclinic crystal system with a P1 space group. The two complexes exhibited similar cytotoxicity level in the panel of cell lines studied with IC50 values between 1.08 and 4.83 µM which is different from previously reported enantiomeric ruthenium and platinum complexes. Electrochemical characterization support compound stability. The compounds also exhibited stability in biological media over 48 hours and has an inert reactivity towards glutathione at 37 oC. These findings provide a new scaffold for the development of new classes of gold-based anticancer agents.

Au(III) complexes with Quinox P* ligand exhibit potent antiproliferative properties

ACS Spring 2022

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