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Radioiodination and biological distribution of a new s ‐triazine derivative for tumor uptake evaluation
Author(s) -
Motaleb Mohamed A.,
Ibrahim Ismail T.,
Sarhan Mona O.,
Zaghary Wafaa A.
Publication year - 2018
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3682
Subject(s) - chemistry , biodistribution , triazine , tris , derivative (finance) , in vitro , ic50 , stereochemistry , docking (animal) , pharmacology , combinatorial chemistry , cancer research , biochemistry , organic chemistry , medicine , nursing , economics , financial economics , biology
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.