Dendritic encapsulation of radiometals by glcydendrimers having a cyclam-core

The dendritic encapsulation of radionuclides opens a promising way for the development of novel imaging and therapeutic agents. On the one side, there is the opportunity to enhance the stability of the encapsulated radionuclide by increasing generation of the dendrimer. Most importantly, the biodistribution can be influenced by grafting a multitude of suitable biomolecules on the periphery of the dendritic skeleton. Recently, we could show that the grafting of polyethylene glycol arms on the cyclam core leads to both a higher complex stability and an increasing shielding effect for copper(II).
In this contribution the synthesis of two novel glycodendrimers 1 and 2 having a cyclam-core (cf. Fig. 1) will be presented. The complex formation of these glycodendrimers with copper(II) has been studied by UV-VIS and time-resolved laser-induced fluorescence (TRLFS) measurements showing the formation of stable 1:1 complexes.
The metal complexes of these water-soluble glycodendrimers appear very attractive in view of binding of the diagnostically and therapeutically relevant radionuclides ^64/67Cu, ^99mTc and ^186/188Re.