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Molecules 2010, 15(12), 8723-8733; doi:10.3390/molecules15128723
Article

Synthesis and Biological Evaluation of Pyrazolo[1,5-a]-pyrimidine-containing 99mTc Nitrido Radiopharmaceuticals as Imaging Agents for Tumors

, , , , , , *  and
Key Laboratory of Radiopharmaceuticals, College of Chemistry, Beijing Normal University, Beijing 100875, China
* Author to whom correspondence should be addressed.
Received: 1 November 2010 / Revised: 15 November 2010 / Accepted: 24 November 2010 / Published: 30 November 2010
(This article belongs to the Section Medicinal Chemistry)
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Abstract

The compound 5-((2-aminoethylamino)methyl)-7-(4-bromoanilino)-3-cyano-pyrazolo[1,5-a]pyrimidine (ABCPP) was synthesized and conjugated with N-mercapto-acetylglycine (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-to-muscle (T/M) ratios and fast clearance from blood and muscle. Among them, the 99mTcN-MAG-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).
Keywords: pyrazolo[1,5-a]pyrimidine; tumor imaging; [99mTcN]2+ complex pyrazolo[1,5-a]pyrimidine; tumor imaging; [99mTcN]2+ complex
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Ding, R.; He, Y.; Xu, J.; Liu, H.; Wang, X.; Feng, M.; Qi, C.; Zhang, J. Synthesis and Biological Evaluation of Pyrazolo[1,5-a]-pyrimidine-containing 99mTc Nitrido Radiopharmaceuticals as Imaging Agents for Tumors. Molecules 2010, 15, 8723-8733.

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