Design of Functional Chiral Cyclen-Based Radiometal Chelators for Theranostics

A series of water-soluble chiral cyclen-based chelators with chemical handles for selective targeting have been synthesized (cyclen = 1,4,7,10-Tetraazacyclododecane). Optical studies, relaxivity measurements, and competitive titrations were performed to show the versatility these chelators. The complexations L3, L4, L5 Lu3+, Y3+, Sc3+, Cu2+ successfully demonstrated in around 90% 100% yields. Efficient rapid radiolabeling 177Lu was achieved under mild conditions 96% yield. exhibit near quantitative labeling efficiencies a wide range radiometal ions, which are promising development specific radiopharmaceutical molecular magnetic resonance imaging contrast agents.