Next Article in Journal
Effects of Conventional Heating on the Stability of Major Olive Oil Phenolic Compounds by Tandem Mass Spectrometry and Isotope Dilution Assay
Previous Article in Journal
Computational Aspects of Carbon and Boron Nanotubes
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
Received: 1 November 2010 / Revised: 15 November 2010 / Accepted: 24 November 2010 / Published: 30 November 2010
(This article belongs to the Section Medicinal Chemistry)
Download PDF [223 KB, uploaded 18 June 2014]

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.

Share & Cite This Article

Further Mendeley | CiteULike
Export to BibTeX |
EndNote
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.

View more citation formats

Related Articles

Article Metrics

For more information on the journal, click here

Comments

Cited By

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert