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

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 successfu...

Descripción completa

Detalles Bibliográficos
Autores principales: Ding, Rui, He, Yong, Xu, Jingli, Liu, Hang, Wang, Xiao, Feng, Man, Qi, Chuanmin, Zhang, Junbo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2010
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6259132/
https://www.ncbi.nlm.nih.gov/pubmed/21119567
http://dx.doi.org/10.3390/molecules15128723
Descripción
Sumario: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 [(99m)TcN](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 (99m)TcN-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).

Ejemplares similares