Gold (III) complexes have emerged as promising chemotherapeutic agents due to their structural versatility, unique redox behavior, and ability to interact with diverse intracellular targets. This mini review highlights recent developments in the design and biological evaluation of gold(III) compounds bearing isoquinoline alkaloids, Schiff base, phosphine, and chiral ligands. These complexes exhibit significant antitumor activities through mechanisms including mitochondrial dysfunction, reactive oxygen species (ROS) generation, and thioredoxin reductase inhibition. Structure–activity relationship (SAR) insights emphasize the role of ligand modification in enhancing complex stability, cellular uptake, and selectivity toward cancer cells. The integration of chiral ligands and bioorthogonal activation strategies further expands the therapeutic scope of gold-based agents. Overall, these findings underscore the potential of gold(III/I) complexes as a versatile platform for next-generation anticancer drug development.