A Click procedure with heterogeneous copper to tether technetium-99m chelating agents and rhenium complexes. Evaluation of the chelating properties and biodistribution of the new radiolabelled glucose conjugates

作者：Benoist Eric^*; Coulais Yvon; Almant Mehdi; Kovensky Jose; Moreau Vincent; Lesur David; Artigau Marine; Picard Claude; Galaup Chantal; Gouin Sebastien G

来源：Carbohydrate Research, 2011, 346(1): 26-34.

DOI：10.1016/j.carres.2010.10.011

• Glycoconjugates
• Heterogeneous click chemistry
• Bioconjugation
• Metal complexes

An efficient protocol was developed to tether chelating agents and rhenium complexes onto a glucoside scaffold with a heterogeneous copper catalyst via click chemistry. The supported catalyst avoids the formation of unwanted copper complexes during the cyclisation step. The possibility to graft a pre-chelated M(CO)(3) core by click chemistry onto a biomolecule was highlighted for the first time. Tc-99m(CO)(3)-glucoconjugates displayed excellent in vitro stability, a fast in vivo blood clearance and a low specific organ uptake or long-term retention in spleen and stomach.

• 出版日期2011-1-3