Radioiodination and biological distribution of a new s-triazine derivative for tumor uptake evaluation.
Mohamed Abd El-MotalebIsmail T IbrahimMona O SarhanWafaa A ZagharyPublished in: Journal of labelled compounds & radiopharmaceuticals (2018)
A newly synthesized s-triazine derivative 1,1',1″-(((1,3,5-triazine-2,4,6-triyl) tris (azanediyl)) tris (benzene-4,1-diyl))tris (ethan-1-one), (1), was synthesized as a part of an ongoing research for development of novel s-triazine-based radiopharmaceuticals. In-vitro cell viability assay against different human cancer cell lines showed very promising inhibitory activity of the synthesized compound. This finding encouraged the radioiodination of 1 to study the degree of its localization in tumor site for evaluating the possibility of its use as a tumor imaging agent. The biodistribution study showed good localization of the radioiodinated derivative 2 at tumor site following i.v. administration in solid tumor-bearing mice. Finally, in a trial to understand the mechanism of the anticancer effect exerted by 1, a target prediction study and a docking study were performed. The results of the first study showed that focal adhesion kinase is a possible target for compound 1 and the docking study confirmed successful binding of both compound 1 and its radioiodinated derivative 2 to the binding site of focal adhesion kinase. As a conclusion, the results of this study suggest that, compound 2 could be used as a potential agent for tumor imaging after preclinical trials.
Keyphrases
- randomized controlled trial
- high resolution
- stem cells
- molecular dynamics
- computed tomography
- small molecule
- mass spectrometry
- climate change
- metabolic syndrome
- mesenchymal stem cells
- young adults
- cystic fibrosis
- pseudomonas aeruginosa
- staphylococcus aureus
- skeletal muscle
- single cell
- positron emission tomography
- water soluble
- placebo controlled