Non-Cross-Bridged Tetraazamacrocyclic Chelator for Stable 64Cu- Based Radiopharmaceuticals

摘要

N-mono/dimethylated TE2A tetraazamacrocycles (MM-TE2A and DM-TE2A) were synthesized in high yields. Both Cu-MM/DM-TE2A complexes showed increased kinetic stability compared to that of Cu-TE2A, whereas Cu- DM-TE2A showed even higher in vitro stability than that of Cu-ECB-TE2A. MM-TE2A and DM-TE2A were quantitatively radiolabeled with ~(64)Cu ions and showed rapid clearance from the body to emerge as a potential efficient bifunctional chelator.