Department of Applied Biology and Chemical Technology, State Key Laboratory of Chemical Biology and Drug Discovery, The Hong Kong Polytechnic University, Hung Hom 999077, Hong Kong SAR.
Department of Medicine, University of Pittsburgh, Pittsburgh, Pennsylvania 15261, United States.
Inorg Chem. 2021 May 17;60(10):7082-7088. doi: 10.1021/acs.inorgchem.0c03734. Epub 2021 Mar 9.
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 Lu, Y, Sc and Cu were successfully demonstrated in around 90% to 100% yields. Efficient and rapid radiolabeling of L5 with Lu 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.
已经合成了一系列具有化学接头的水溶性手性环戊烷基螯合剂，用于选择性靶向（环戊烷= 1,4,7,10-四氮杂环十二烷）。进行了光学研究、弛豫率测量和竞争性滴定，以显示这些手性螯合剂的多功能性。L3、L4 和 L5 与 Lu、Y、Sc 和 Cu 的络合反应以 90%至 100%的产率成功证明。在温和条件下，L5 与 Lu 的放射性标记以 96%的产率高效且快速进行。这些螯合剂与多种放射性金属离子表现出接近定量的标记效率，这对于开发针对特定放射性药物和分子磁共振成像造影剂的靶向具有广阔的前景。
