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

第三代潜在双功能三硫醇螯合物、其天然 1XXSb(III) 复合物及其与 Sn 靶标的放射性锑 (119Sb) 的选择性螯合

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作者:Aeli P Olson, Li Ma, Yutian Feng, Firouzeh Najafi Khosroshahi, Steven P Kelley, Eduardo Aluicio-Sarduy, Todd E Barnhart, Heather M Hennkens, Paul A Ellison, Silvia S Jurisson, Jonathan W Engle

Abstract

The therapeutic potential of the Meitner-Auger- and conversion-electron emitting radionuclide 119Sb remains unexplored because of the difficulty of incorporating it into biologically targeted compounds. To address this challenge, we report the development of 119Sb 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 119Sb-trithiol complex has high stability and can be purified by HPLC. The third generation trithiol chelate and the analogous stable natSb-trithiol compound were synthesized and characterized, including by single-crystal X-ray diffraction analyses.

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