American Chemical Society
ic1c00415_si_001.pdf (1.42 MB)

Potent PBS/Polysorbate-Soluble Transplatin-Derived Porphyrin-Based Photosensitizers for Photodynamic Therapy

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journal contribution
posted on 2021-06-11, 17:40 authored by Lukas Schneider, Martina Kalt, Michele Larocca, Vipin Babu, Bernhard Spingler
In this study, we addressed an important drawback of our previously reported tetraplatinated (metallo)­porphyrin-based photosensitizers (PSs) for photodynamic therapy (PDT), namely, the poor solubility in aqueous media. We aimed to create tetraplatinated porphyrin-based PSs that are soluble in aqueous media modified with polysorbate (Tween) and do not need to be pre-dissolved in organic solvents. A structural optimization of the previously reported PSs resulted in the synthesis of an extremely potent novel porphyrin-based PS. The novel PS displays effective phototoxicity upon light irradiation against multicellular tumor spheroids and has a phototoxic index (PI) of 6030 in HeLa cells. This PI value is, to the best of our knowledge, the highest value reported for any porphyrin so far.