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 |
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页(从-至) | 5288-5294 |
页数 | 7 |
期刊 | Journal of Medicinal Chemistry |
卷 | 56 |
期 | 13 |
DOI | |
出版状态 | 已出版 - 11 7月 2013 |
已对外发布 | 是 |