Synthesis and in Vitro Photocytotoxicity of Coumarin Derivatives for One- and Two-Photon Excited Photodynamic Therapy

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• 作者：Qianli Zou ; Yanyan Fang ; Yuxia Zhao ; Hongyou Zhao ; Ying Wang ; Ying Gu ; Feipeng Wu
• 刊名：Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：July 11, 2013
• 年：2013
• 卷：56
• 期：13
• 页码：5288-5294
• 全文大小：371K
• 年卷期：v.56,no.13(July 11, 2013)
• ISSN：1520-4804

文摘

Triethylene glycol functionalized coumarin derivatives 1鈥?b>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鈥損roperty 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.