Department of Medical Physics, University of Wisconsin, Madison, Wisconsin 53705, United States.
Department of Chemistry, University of Missouri, Columbia, Missouri 65211, United States.
Inorg Chem. 2021 Oct 18;60(20):15223-15232. doi: 10.1021/acs.inorgchem.1c01690. Epub 2021 Oct 4.
The therapeutic potential of the Meitner-Auger- and conversion-electron emitting radionuclide Sb remains unexplored because of the difficulty of incorporating it into biologically targeted compounds. To address this challenge, we report the development of Sb production from electroplated tin cyclotron targets and its complexation by a novel trithiol chelate. The chelation reaction occurs in harsh solvent conditions even in the presence of large quantities of tin, which are necessary for production on small, low energy (16 MeV) cyclotrons. The Sb-trithiol complex has high stability and can be purified by HPLC. The third generation trithiol chelate and the analogous stable Sb-trithiol compound were synthesized and characterized, including by single-crystal X-ray diffraction analyses.
由于难以将其掺入生物靶向化合物中，因此梅特纳-俄歇和转换电子发射放射性核素 Sb 的治疗潜力尚未得到探索。为了解决这一挑战，我们报告了从电镀锡回旋加速器靶材中生产 Sb 并通过新型三硫醇螯合物对其进行络合的方法。即使在存在大量锡（对于在小的低能（16 MeV）回旋加速器上进行生产是必需的）的苛刻溶剂条件下，也会发生螯合反应。Sb-三硫醇配合物具有高稳定性，并且可以通过 HPLC 进行纯化。合成并表征了第三代三硫醇螯合物和类似的稳定 Sb-三硫醇化合物，包括通过单晶 X 射线衍射分析。
