Molecules p. 8723 - 8733 (2010)
Update date:2022-08-05
Topics:
Ding, Rui
He, Yong
Xu, Jingli
Liu, Hang
Wang, Xiao
Feng, Man
Qi, Chuanmin
Zhang, Junbo
The compound 5-((2-aminoethylamino)methyl)-7-(4-bromoanilino)-3- cyanopyrazolo[ 1,5-a]pyrimidine (ABCPP) 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 tumor accumulation, high tumor-tomuscle (T/M) ratios and fast clearance from blood and muscle. Among them, the 99mTcNMAG-ABCPP showed the most favorable characteristics, with tumor/blood and tumor/muscle ratios reaching 1.51 and 2.97 at 30 min post-injection, 1.84 and 2.49 at 60 min post-injection, suggesting it could be further studied as potential tumor imaging agent for single photon emission computed tomography (SPECT).
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Doi:10.1016/j.ica.2010.08.052
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