Abstract
The 7-(2-aminoethylamino)-5-methyl-3-cyanopyrazolo[1,5-a]pyrimidine (AMCPP) was synthesized and conjugated with N-mercaptoacetylglycine (MAG), N-mercaptoacetylphenylalanine (MAF), and N-mercaptoacetylvaline (MAA), respectively. These three compounds were labeled successfully with [99mTcN]2+ intermediate in high radiochemical purities. Biodistribution in tumor-bearing mice demonstrated that the three new complexes showed high tumor-to-muscle (T/M) ratios and rapid clearance from the blood, muscle, liver, kidney, and lung. Among them, the 99mTcN-MAG-AMCPP showed the most favorable characteristics. The tumor/blood and tumor/muscle ratios reached 1.50 and 1.15 at 30 min post-injection, 2.20 and 1.83 at 60 min post-injection.
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Acknowledgments
The study was financially supported by National Natural Science Foundation of China (no 20371009 and 20671014) and Beijing Key Subject Program. We also wish to thank Beijing Municipal Commission of Education.
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Ding, R., He, Y., Xu, J. et al. Preparation and bioevaluation of 99mTc nitrido radiopharmaceuticals with pyrazolo[1,5-a]pyrimidine as tumor imaging agents. Med Chem Res 21, 523–530 (2012). https://doi.org/10.1007/s00044-011-9558-8
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DOI: https://doi.org/10.1007/s00044-011-9558-8