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Molecules 2018, 23(6), 1436;

Synthesis and Evaluation of New Potential Benzo[a]phenoxazinium Photosensitizers for Anticancer Photodynamic Therapy

School of Biological Science and Technology, University of Jinan, Jinan 250022, China
Faculty of Ceilandia, University of Brasília, Brasilia 72220275, Brazil
Institute of Biological Sciences, University of Brasília, Brasilia 70910900, Brazil
Authors to whom correspondence should be addressed.
Received: 16 May 2018 / Revised: 31 May 2018 / Accepted: 8 June 2018 / Published: 13 June 2018
(This article belongs to the Special Issue Advances in Photodynamic Therapy 2018)
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The 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
Keywords: benzo[a]phenoxazinium; photosensitizer; reactive oxygen species; photodynamic therapy; anticancer benzo[a]phenoxazinium; photosensitizer; reactive oxygen species; photodynamic therapy; anticancer

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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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.

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