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Water-soluble cyclodextrin (CyD) complexed with porphyrin derivatives with different substituents in the meso -positions showed different photodynamic activities toward cancer cells under illumination at wavelengths over 600 nm, the most suitable wavelengths for photodynamic therapy (PDT). In particular, aniline- and phenol-substituted derivatives had high photodynamic activity because of the efficient intracellular uptake of the complexes by tumor cells. These complexes showed greater photodynamic activity than photofrin, currently the main drug in clinical use as a photosensitizer. These results represent a significant step toward the optimization of porphyrin derivatives as photosensitizers.

Photodynamic Activities of Porphyrin Derivative–Cyclodextrin Complexes by Photoirradiation