4.7 Article

A Third Generation Potentially Bifunctional Trithiol Chelate, Its nat,1XXSb(III) Complex, and Selective Chelation of Radioantimony (119Sb) from Its Sn Target

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INORGANIC CHEMISTRY
卷 60, 期 20, 页码 15223-15232

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AMER CHEMICAL SOC
DOI: 10.1021/acs.inorgchem.1c01690

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资金

  1. NIH T32 NRSA Institutional Predoctoral Training Fellowship [2T32CA00920641]
  2. NIH F31 Ruth L Kirschstein Predoctoral Individual National Research Service Award [F31CA239617]
  3. NIH NCI [P01CA250972]
  4. U.S. Department of Energy Isotope Program [DE-SC0010283, DE-SC0020159]
  5. U.S. Department of Energy (DOE) [DE-SC0020159, DE-SC0010283] Funding Source: U.S. Department of Energy (DOE)

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A new trithiol chelate was developed in this study to successfully complex with Sb-119, which can be purified by HPLC. This method provides a solution to the challenge of incorporating Sb-119 into biologically targeted compounds.
The therapeutic potential of the Meitner-Auger- and conversion-electron emitting radionuclide Sb-119 remains unexplored because of the difficulty of incorporating it into biologically targeted compounds. To address this challenge, we report the development of Sb-119 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-119-trithiol complex has high stability and can be purified by HPLC. The third generation trithiol chelate and the analogous stable Sb-nat-trithiol compound were synthesized and characterized, including by single-crystal X-ray diffraction analyses.

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