Gold-based compounds are gaining attention as potential alternatives to platinum-based chemotherapeutics due to their high antiproliferative activity and unique mechanisms of action. However, challenges remain in enhancing their selectivity and reducing side effects. In this study, we synthesized and characterized a series of gold(I) azido complexes featuring phosphine and N-heterocyclic carbene ligands. Their cytotoxicity was assessed against human lung carcinoma (A549) and non-cancerous fibroblast (MRC-5) cells, revealing micromolar-range antiproliferative effects with varying selectivity. Additionally, their use as photoactivated chemotherapy (PACT) agents was explored, with some complexes displaying modulation of their cytotoxicity upon light exposure. These findings suggest that gold azido complexes could serve as promising drug candidates for chemotherapy treatments.