Through the use of a rhodamine appended chelate, a versatile strategy has been demonstrated to generate mitochondria-targeting photosensitizers via the incorporation of variety of luminescent transition metal systems. The generation of triplet excited state of rhodamine moiety endows the complexes with mitochondria-targeting photosensitizing ability to form singlet oxygen (1O2) for use as photodynamic therapy (PDT) agent. The combination of rhodamine organic dye and luminescent transition metal centers in such hybrid systems exhibits the synergistic merits, including low dark cytotoxicity, selective tumor cell uptake, high molar absorptivity for low-energy excitation in the visible region, and high photostability.