Di-macrocyclic terephthalamide ligands as chelators for the PET radionuclide zirconium-89

Abstract

The development of bifunctional chelators (BFCs) which can stably chelate zirconium-89 (⁸⁹Zr) while being conjugated to targeting molecules is an area of active research. Herein we report the first octadentate terephthalamide ligands, which are easily radiolabeled with ⁸⁹Zr and are highly stable in vitro. They represent a novel class of chelators, which are worthy of further development as BFCs for ⁸⁹Zr.