Synthesis and biological evaluation of novel 99mTc(CO)3 labeled glucose derivatives prepared by click chemistry route

Abstract

In this study, two novel C-1 functionalized glucose derivatives containing 1, 2, 3-triazoles (3a and 3b) were synthesized via a copper catalyzed azide–alkyne cyclization reaction. The ligands were successfully radiolabeled with [99mTc(CO)3(H2O)3]+ to produce 99mTc(CO)3-3a and 99mTc(CO)3-3b. Both complexes were prepared with high radiochemical purity and had good in vitro stability. The partition coefficient results showed they were hydrophilic. The in vivo biodistribution studies in mice bearing S 180 tumor showed that both complexes accumulated in the tumor with high uptake and good retention. The high tumor uptake together with favorable tumor-to-muscle ratios make them candidates for further evaluation as promising tumor imaging tracers.