Journal
INORGANICA CHIMICA ACTA
Volume 520, Issue -, Pages -Publisher
ELSEVIER SCIENCE SA
DOI: 10.1016/j.ica.2021.120291
Keywords
Tridentate ligands; Rhenium complexes; X-ray crystallography; Fac-[Re(CO)3L]n
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Funding
- Kentucky Biomedical Research Infrastructure Network (KBRIN) [P20GM103436]
- EKU University Research Grant
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The research aims to develop new rhenium complexes for use in radiometal complexes or for conjugation with biomolecules to create targeted radiolabelled biopharmaceuticals. The study focused on designing and synthesizing water-soluble rhenium complexes, and characterizing their metal binding to biomolecules using various analytical techniques.
The aim of this research is to develop new rhenium complexes with favorable bio-distribution properties which can be used as radiometal complexes or for conjugation with biomolecules for the development of targeted radiolabelled biopharmaceuticals. Two metals of interest utilized in radiopharmaceuticals are technetium and rhenium, both of which share similar chemical and structural properties. The coordination chemistry of these metals is highly dependent upon ligands that are structurally and chemically robust among other factors. The synthesis of new symmetrical tridentate ligands and ligand conjugation methods will expand the likelihood of developing suitable fac-[Re(CO)3L]n compounds with promising biomedical properties and were consequently the subject of this investigation. In order to accomplish this, the design, synthesis, characterization and X-ray structure of new water-soluble rhenium complexes for assessing metal binding to biomolecules were investigated. Three diethylenetriamine (dien) derivatives, 2-(bis(2-aminoethyl)amino)-N-(2-oxo-4-(trifluoromethyl)2H-chromen-7-yl)acetamide (atfcdien, 3), 2-(bis(2-aminoethyl)amino)-N-(3,5-bis(trifluoromethyl)benzyl)acetamide (tfmedien, 6), and N-benzyl-2-(bis(2-aminomethyl)amino)acetamide (badien, 9) and their rhenium complexes were synthesized. 1H NMR spectroscopy, mass spectrometry and X-ray crystallography techniques were employed to characterize the ligands and their rhenium complexes [Re(CO)3atfcdien]Br (10), [Re (CO)3tfmedien]Br (11) and [Re(CO)3badien]Br (12). 1H NMR studies were conducted to examine chelated Re complexes revealed a consistent downfield shift of the CH signal of the dien moiety for all three new ligands.
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