Synthesis and in vitro photocytotoxicity of coumarin derivatives for one- and two-photon excited photodynamic therapy

Qianli Zou, Yanyan Fang, Yuxia Zhao*, Hongyou Zhao, Ying Wang, Ying Gu, Feipeng Wu

*此作品的通讯作者

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摘要

Triethylene glycol functionalized coumarin derivatives 1-5 were synthesized and investigated as photosensitizers for one- and two-photon excited photodynamic therapy (PDT). Their absorption, fluorescence, triplet-state quantum yields, and singlet oxygen quantum yields were found to be significantly related to the substituent at the 7-position of the coumarin ring. In vitro photocytotoxicity of these derivatives toward HepG2 cells was examined and compared with a clinical drug. In vitro generation of reactive oxygen species (ROS), cellular uptake, and intracellular distribution of these derivatives were also characterized to fully reveal their structure-property relationships. The results showed that derivative 5, with a two-photon absorption cross section value of 1556 GM, could be a powerful PDT agent for both superficial diseases and solid tumors.

源语言英语
页(从-至)5288-5294
页数7
期刊Journal of Medicinal Chemistry
56
13
DOI
出版状态已出版 - 11 7月 2013
已对外发布

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Zou, Q., Fang, Y., Zhao, Y., Zhao, H., Wang, Y., Gu, Y., & Wu, F. (2013). Synthesis and in vitro photocytotoxicity of coumarin derivatives for one- and two-photon excited photodynamic therapy. Journal of Medicinal Chemistry, 56(13), 5288-5294. https://doi.org/10.1021/jm400025g