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).
Highlights
Tumors are among the most common causes of death in the World
The use of pyrazolo[1,5-a]pyrimidine derivatives as antitumor agents for the treatment of cancer has come under much attention in a growing number of therapeutic areas [1,2,3,4,5,6]
It may be of great interest to probe the 99mTc nitrido chemistry with some ligands involving the ABCPP molecular structure to explore the biological behaviour of a potential new class of diagnostic agents
Summary
Tumors are among the most common causes of death in the World. Recently, the use of pyrazolo[1,5-a]pyrimidine derivatives as antitumor agents for the treatment of cancer has come under much attention in a growing number of therapeutic areas [1,2,3,4,5,6]. 3-cyano-5,7disubstistituted pyrazolo[1,5-a]pyrimidine derivatives showed significant antitumor properties [7,8]. The nitrido ligand is a powerful -electron donor and shows a high capacity to stabilize the Tc(V) oxidation state [9]. The presence of the [99mTcN]2+ core in the molecular structure of a radiopharmaceutical may dramatically affect its physical and biological behaviour [10]. The use of the 3-cyano-5,7-disubstistituted pyrazolo[1,5-a]pyrimidine moiety in the preparation of 99mTcN complexes as targeted agents for tumor imaging has not been reported. It may be of great interest to probe the 99mTc nitrido chemistry with some ligands involving the ABCPP molecular structure to explore the biological behaviour of a potential new class of diagnostic agents
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
