Highly inert Cu() complexes of -aryl bifunctional cyclam-picolinates with remarkable Cu-labelling and biodistribution

Cyclam-picolinate chelators were functionalized via click chemistry with an additional carboxyl group for subsequent bioconjugation to antibodies or for the modification of the overall charge of the corresponding 64 Cu-radiocomplexes. The C -aryl functionalization strategy developed here preserves the chemical properties of the radiocomplexes whilst deeply enhancing their applications within nuclear medicine. Two bifunctional copper chelators H 2 TE1PA-trz-prA and H 2 CB-TE1PA-trz-prA were synthesized and their relevant nat Cu- and 64 Cu-complex properties highlighted.