BODIPY-Based Photothermal Agents with Excellent Phototoxic Indices for Cancer Treatment

• DOI: 10.1021/jacs.2c11650
• Publication Date: 2023-02-13T18:19:50Z
• Authors: Lukas Schneider; Martina Kalt; Samuel Koch; Shanmugi Sithampa...; Veronika Villiger; Johann Mattiat; Flavia Kradolfer; Ekaterina Slyshkina; Sandra Luber; Mathias Bonmarin; Caroline Maake; Bernhard Spingler
• Keywords: Phototoxicity; BODIPY; Therapeutic index; Photothermal effect

Here, we report six novel, easily accessible BODIPY-based agents for cancer treatment. In contrast to established photodynamic therapy (PDT) agents, these compounds show additional photothermal activity and their cytotoxicity is not dependent on the generation of reactive oxygen species (ROS). The high photocytotoxicity upon irradiation with light low dark toxicity in different cell lines 2D culture as well 3D multicellular tumor spheroids (MCTSs). ratio (phototoxic index, PI) reaches striking values exceeding 830,000 after energetically doses at 630 nm. oxygen-dependent mechanism action (MOA) photosensitizers (PSs) hampers effective clinical deployment agents. Under hypoxic conditions (0.2% O2), which are known limit efficiency conventional PSs solid tumors, was induced same concentration levels, indicating an oxygen-independent MOA. With a PI 360,000 under conditions, both highest reported date. We anticipate that small molecule MOA, such this work, may overcome barrier provide new avenue therapy.