Amino acid derivatives of pyropheophorbide-α ethers as photosensitizer: Synthesis and photodynamic activity |
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| Authors: | Zhi Meng Bin Shan Ling Zhang Gui-Yan Han Ming-Hui Liu Ning-Yang Jia Zhen-Yuan Miao Wan-Nian Zhang Chun-Quan Sheng Jian-Zhong Yao |
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| Institution: | a Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China;
b Department of Pharmacy, Fujian University of Traditional Chinese Medicine, Fuzhou 350122, China;
c Department of Radiology, Shanghai Eastern Hepatobiliary Surgery Hospital, Second Military Medical University, Shanghai 200438, China |
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| Abstract: | Ten new water-soluble amino acid conjugates of pyropheophorbide-α ethers 4a-4j were synthesized and investigated for their in vitro photodynamic antitumor activity. The results showed that all compounds exhibited higher phototoxicity and lower dark toxicity against three kinds of tumor cell lines than BPD-MA. In particular, themost phototoxic compound 4d and 4j individually showed IC50 values of 41 nmol/L and 33 nmol/L against HCT116 cell, which represented 7.8- and 9.7-fold increase of antitumor potency compared to BPD-MA, respectively, suggesting that they were promising photosensitizers for PDT applications because of their strong absorption at long wavelength (λmax>650 nm), high phototoxicity, low dark cytotoxicity and good water-solubility. |
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| Keywords: | Photodynamic therapy (PDT) Photosensitiser Pyropheophorbide-α Chlorin Antitumor |
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