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The initiation and propagation of cancer is closely associated with bacterial infection, which generally requires the simultaneous usage of anticancer drugs and antibiotics. However, the adverse effects have increased too much due to the multiple use of chemodrugs. To tackle this problem, a successful attempt has been made by developing two BODIPY-based cationic photosensitizers, 1BDPC-Py and 1BDPC-TPP, for treating both cancer and bacterial infection. Optimization of the basic design of these photosensitizers resulted in the red-light absorption, improved ¹O₂ generation yield, outstanding therapeutic effects and optical physical properties for excellent imaging. The decorated cationic groups grant some highly favorable features, such as a mediated hydrophilic-lipophilic balance for improving cell penetrability, specific mitochondrial anchoring for enhanced PDT and the increased attraction towards bacterial …