Title: Design of functional chiral cyclen-based radiometal chelators for theranostics
Authors: Dai, L 
Zhang, J 
Wong, CT 
Chan, WTK 
Ling, X
Anderson, CJ
Law, GL 
Issue Date: 2021
Source: Inorganic chemistry, 2021, https://doi.org/10.1021/acs.inorgchem.0c03734
Abstract: 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 of these chiral chelators. The complexations of L3, L4, and L5 with Lu3+, Y3+, Sc3+, and Cu2+ were successfully demonstrated in around 90% to 100% yields. Efficient and rapid radiolabeling of L5 with 177Lu was achieved under mild conditions with 96% yield. The chelators exhibit near quantitative labeling efficiencies with a wide range of radiometal ions, which are promising for the development of targeting specific radiopharmaceutical and molecular magnetic resonance imaging contrast agents.
Publisher: American Chemical Society
Journal: Inorganic chemistry 
ISSN: 0020-1669
DOI: 10.1021/acs.inorgchem.0c03734
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