Abstract

AbstractAn activatable photosensitizer for singlet oxygen is of significance due to its potential application in tumor‐specific photodynamic therapy and diagnosis. In this study, a pH‐activatable system that enables the specific photosensitization of singlet oxygen at a low pH value was developed based on the complexation of a porphyrin‐aniline conjugate with phosphorus(V). As a result of complexation with phosphorus, the water solubility of the porphyrin‐aniline conjugate was improved 100‐fold. Furthermore, this complexation strongly suppressed the singlet‐oxygen‐generating activity of the porphyrin photosensitizer under basic conditions, and the quantum yield of the singlet oxygen photosensitization markedly increased under acidic conditions. Based on these improvements, an extremely high ON/OFF switching ratio of the quantum yield was obtained (>400‐fold).

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