Preparation, characterization, and biological evaluation of technetium(V) and rhenium(V) complexes of novel heterocyclic tetradentate N3S ligands

Bioconjugate Chemistry
R RajagopalanA Srinivasan

Abstract

Various tetradentate N3S ligands which contain pyridyl, morpholino, or imidazolyl moieties were prepared and labeled with technetium and rhenium. Metal complexation of the ligands occurred efficiently over the pH range from 2 to 11. Ligands possessing the S-THP (tetrahydropyranyl)-protected mercapto group labeled efficiently even under alkaline conditions, and among the three types of heterocyclic metal complexes, a marked difference in stability was observed; rhenium complexes decomposed to ReO4 whereas technetium complexes decomposed to TcO2/TcO4. In general, imidazolyl complexes of both technetium and rhenium were very stable in saline; less than 10% decomposition after 24 h. The technetium histidyl complex and technetium pyridyl complex were quite stable even under cysteine challenge; less than 10% decomposition after 24 h. The rhenium and technetium morpholino complexes were very unstable; greater than 10% decomposition after only 1 h in saline and greater than 25% decomposition in 1 h under cysteine challenge. Profound pharmacokinetic differences among these metal complexes were also observed in rat biodistribution studies. The neutral pyridyl complexes exhibited high blood and liver uptake and slow clearance from these t...Continue Reading

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Citations

Feb 26, 2015·Dalton Transactions : an International Journal of Inorganic Chemistry·Jonathan R DilworthClaudiu T Supuran
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