Cyclometalated Iridium(III) Complexes as Mitochondria‐targeting Photosensitizers against Cisplatin‐resistant Cells†

Four iridium (III) complexes Ir1-Ir4 were synthesized and characterized. Possessing high singlet oxygen production ability and specific mitochondria-localization, Ir1 was developed as a mitochondria-targeting photosensitizer. Ir1 exhibited strong phototoxicity against cancer cell line A549 and its corresponding cisplatin-resistant one A549R. In contrast, Ir1 showed low cytotoxicity toward normal cell HLF. This selectivity resulted from the different uptake amount. With 405 nm irradiation, Ir1 induced mitochondria-mediated cell death in A549R cells, achieving the overcome of drug-resistant.