Photodynamic therapy has been established as one of the approaches for the treatment of various malignant tumors. While most of the reagents used for this purpose are porphyrin derivatives, there is a strong motivation for finding novel and better sensitizers. Perylenediimides are known for their photo- and chemical stability, but they do not have absorptions in the red end of the visible spectrum. However, recently reported green perylenediimides which have dialkylamino substituents on the perylene core, provide an alternative. To that end, we have designed and synthesized novel green perylenediimides with remarkable water solubility at neutral pH and absorption peaks beyond 650 nm. We demonstrated that on red-light excitation, singlet oxygen trap 1,3-diphenyl-iso-benzofuran is rapidly degraded. We also carried out cell culture experiments / an important parameter to be optimized for practical application as a novel photodynamic therapy agent was the excited dye toxicity to dark toxicity. Our results confirmed that these novel perylenediimides acted as sensitizers generating singlet oxygen and the initial in vitro biological experiments demonstrated their potential utility in photodynamic therapy.

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