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Date of Publication:2021-01-01

Journal:Jingxi Huagong/Fine Chemicals

Volume:38

Issue:9

Page Number:1875-1880 and 1895

ISSN No.:1003-5214

Abstract:In order to find a photosensitizer with better photodynamic therapy effect, 3-hydroxymethyl- 4-phenyl-1, 2, 5-oxadiazole-2-oxide was synthesized fromcinnamyl alcohol, followed by an esterification reaction of it with chlorin e6 to give a chlorin e6 conjugate containing furoxan (Ⅳ). The structure of the target compound was characterized by HRMS, 1HNMR, 13CNMR and IR. The activity evaluation results showed that the introduction of furoxan group increased 33-fold the uptake rate compared with chlorin e6, increased the level of intracellular NO by 2.3-fold, increased the number of intracellular ROS by 1.3-fold, the level of GSH in the cell was reduced by 26%, and synergistically enhance the photodynamic inhibition of tumor cell proliferation activity by about 20-fold. At 33 μmol/L, the proliferation inhibition rate of compound Ⅳ on Hela cells was 96%. © 2021, Editorial Office of FINE CHEMICALS. All right reserved.

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