Synthesis and evaluation of Diaza-Crown Ether-Backboned chelator containing hydroxamate groups for Zr-89 chelation chemistry

[Display omitted] Zirconium-89 (89Zr) has been explored for molecularly targeted positron emission tomography (PET) imaging of various diseases. We synthesized and evaluated a novel chelator (DA-18C6-BHA) for 89Zr. The new chelator is structured on a macrocyclic backbone (1,10-diaza-18-crown-6) and...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2022-09, Vol.72, p.128847-128847, Article 128847
Main Authors: Zhang, Shuyuan, Wang, Haixing, Ren, Siyuan, Chen, Yanda, Liu, Dijie, Li, Mengshi, Sagastume, Edwin, Chong, Hyun-Soon
Format: Article
Language:English
Subjects:
Chelator
PET Imaging
Zr-89
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Summary:[Display omitted] Zirconium-89 (89Zr) has been explored for molecularly targeted positron emission tomography (PET) imaging of various diseases. We synthesized and evaluated a novel chelator (DA-18C6-BHA) for 89Zr. The new chelator is structured on a macrocyclic backbone (1,10-diaza-18-crown-6) and contains hydroxamates as acyclic donor groups. The new chelator ((DA-18C6-BHA) was rapidly labeled with 89Zr under mild conditions. The 89Zr-labeled DA-18C6-BHA complex remained stable in human serum and apotransferrin for 7 days. When challenged with excess EDTA solution, 89Zr-labeled DA-18C6-BHA was shown to hold 89Zr without losing considerable radioactivity to EDTA. The 89Zr-labeled DA-18C6-BHA complex displayed high complex stability in normal mice as evidenced by low bone uptake.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2022.128847