Design of Functional Chiral Cyclen-Based Radiometal Chelators for Theranostics

Lixiong Dai, Junhui Zhang, Carlos Tinlong Wong, Wesley Ting Kwok Chan, Xiaoxi Ling, Carolyn J. Anderson, Ga Lai Law (Corresponding Author)

Research output: Journal article publicationJournal articleAcademic researchpeer-review

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.

Original languageEnglish
Pages (from-to)7082-7088
Number of pages7
JournalInorganic Chemistry
Volume60
Issue number10
DOIs
Publication statusPublished - 17 May 2021

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Inorganic Chemistry

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