Study on radiolabeling of 1,2,3-triazole analogs with fac-[188Re(CO)3 (H2O)3 ]+ via click chemistry |
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作者姓名: | WANG Cheng YIN Jilin ZHOU Wei ZHANG Lan ZHOU Zheng |
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作者单位: | PET/CT center,General Hospital of Guangzhou Military Command;Shanghai Institute of Applied Physics,Chinese Academy of Sciences,Jiading Campus |
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基金项目: | Supported by National Natural Science Foundation of China(No.10875163);Natural Science Foundation of Guangdong Province(Nos.2009B030108036 and S2012010010685) |
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摘 要: | Click chemistry was used to study on radiolabeling of 1,2,3-triazole analogs with fac-[188 Re(CO) 3 (H 2 O) 3]+ . CuSO 4 /L-sodium ascorbate was chosen as the catalyst system, three terminal alkynes were conjugated with two different azides respectively, and then the new prepared fac-[188 Re(CO) 3 (H 2 O) 3]+ was coordinated to the six triazoles. The results showed that the radiochemical yields (RCY) of the conjugation of fac-[188 Re(CO) 3]+ with six triazoles were over 90%, and the triazoles showed high stability in phosphate-buffered saline and new-born calf serum. The preliminary biological evaluation results showed that the new 188 Re-labeling method via click chemistry could have general application in labeling bioactive molecules in high radiochemical yield and high specific activity for further SPECT research.
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关 键 词: | Tricarbonyl Rhenium-188 Stability Triazole analogs Radiotherapy Click chemistry |
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