Emerging synthetic development of chiral gold(III) complexes has prompted new opportunities in catalysis and material science with limited utility in biomedicine. Here, we demonstrate potential chemotherapeutic capability of [C^N]Au(III)Cl(R-DuPhos) (1-7) complexes, containing 1,2-bis[(2R,5R)-2,5-dialkylphospholano]benzene, which shows good stabilty, potent anticancer activity, and tolerability in mice.