Synthesis and Evaluation of New Potential Benzo[a]phenoxazinium Photosensitizers for Anticancer Photodynamic Therapy
AbstractThe use of photodynamic therapy (PDT) and development of novel photosensitizers (PSs) for cancer treatment have received more and more attention nowadays. In the present work, five benzo[a]phenoxazinium derivatives have been prepared and evaluated for their in vitro anticancer photodynamic activity for the first time. They are red light absorbers and show low fluorescence quantum yield. Of these compounds, PS4 exhibited a higher quantum yield for reactive oxygen species (ROS) generation. The assays with cells in vitro showed that PS1 and PS4 were not significantly toxic in the dark, but was robustly toxic against the murine breast adenocarcinoma cells 4T1 and normal murine fibroblast cells NIH-3T3 upon photoactivation. More interestingly, PS5 was particularly selective towards 4T1 cancer cells and nearly non-phototoxic to non-cancerous NIH-3T3 cells. The results described in this report suggest that these new benzo[a]phenoxazinium derivatives are potential candidates as PSs for anticancer PDT. Further investigation of benzo[a]phenoxaziniums for anticancer PDT is warranted. View Full-Text
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Zhang, J.; Tavares de Sousa Júnior, W.; Mello da Silva, V.C.; Rodrigues, M.C.; Vasconcelos Morais, J.A.; Song, J.-L.; Cheng, Z.-Q.; Longo, J.P.F.; Bentes Azevedo, R.; Jiang, C.-S.; Alexandre Muehlmann, L.; Zhang, H. Synthesis and Evaluation of New Potential Benzo[a]phenoxazinium Photosensitizers for Anticancer Photodynamic Therapy. Molecules 2018, 23, 1436.
Zhang J, Tavares de Sousa Júnior W, Mello da Silva VC, Rodrigues MC, Vasconcelos Morais JA, Song J-L, Cheng Z-Q, Longo JPF, Bentes Azevedo R, Jiang C-S, Alexandre Muehlmann L, Zhang H. Synthesis and Evaluation of New Potential Benzo[a]phenoxazinium Photosensitizers for Anticancer Photodynamic Therapy. Molecules. 2018; 23(6):1436.Chicago/Turabian Style
Zhang, Juan; Tavares de Sousa Júnior, Wellington; Mello da Silva, Victor C.; Rodrigues, Mosar C.; Vasconcelos Morais, José A.; Song, Jia-Li; Cheng, Zhi-Qiang; Longo, João P.F.; Bentes Azevedo, Ricardo; Jiang, Cheng-Shi; Alexandre Muehlmann, Luís; Zhang, Hua. 2018. "Synthesis and Evaluation of New Potential Benzo[a]phenoxazinium Photosensitizers for Anticancer Photodynamic Therapy." Molecules 23, no. 6: 1436.
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