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Three novel gold(III) complexes (<b>1</b>–<b>3</b>) of general composition [Au(Bipydc)(S₂CNR₂)]Cl₂ (Bipydc = 2,2′-bipyridine-3,3′-dicarboxylic acid and R = methyl for dimethyldithiocarbamate (DMDTC), ethyl for diethyldithiocarbamate (DEDTC), and benzyl for dibenzyldithiocarbamate (DBDTC)) have been synthesized and characterized by elemental analysis, FTIR and NMR spectroscopic techniques. The spectral results confirmed the presence of both the Bipydc and dithiocarbamate ligands in the complexes. The in vitro cytotoxic studies demonstrated that compounds <b>1</b>–<b>3</b> were highly cytotoxic to A549, HeLa, MDA-231, and MCF-7 cancer cells with activities much higher (about 25-fold) than cisplatin. In order to know the possible mode of cell death complex <b>2</b>, [Au(Bipydc)(DEDTC)]Cl₂ was further tested for induction of apoptosis towards the MCF-7 cells. The results indicated that complex <b>2</b> induces cell death through apoptosis.