Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development.
نویسندگان
چکیده
We report our initial investigations into the use of tetraazamacrocycles as zirconium-89 chelators. We describe the synthesis and complete characterization of several Zr tetraazamacrocycle complexes, and definitively describe the first crystal structure of zirconium 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (Zr-DOTA) using single crystal X-ray diffraction analysis. After evaluating several radioactive analogs, we found that 89Zr-DOTA is superior to 89Zr-DFO, the only 89Zr-complex to be used clinically in 89Zr-radiopharmaceutical applications. Finally, we provide a rationale for the unanticipated and extraordinary stability of these complexes in vitro and in vivo. These results may inform the development of safer and more robust immuno-PET agents for precision medicine applications.
منابع مشابه
Zirconium tetraazamacrocycle complexes display extraordinary stability and provide a new strategy for zirconium-89-based radiopharmaceutical development† †TJW, DNP and NB have filed patents relating to this work. All other authors declare no competing financial interests exist. ‡ ‡Electronic supplementary information (ESI) available: Complete experimental details and supporting data. CCDC 1501174. For ESI and crystallographic data in CIF or other electronic format see DOI: 10.1039/c6sc04128k Click here for additional data file. Click here for additional data file.
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ورودعنوان ژورنال:
- Chemical science
دوره 8 3 شماره
صفحات -
تاریخ انتشار 2017