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通过与锌衍生物的转金属反应生成的生物缀合锝羰基化合物。

Bioconjugated technetium carbonyls by transmetalation reaction with zinc derivatives.

机构信息

Departament de Química, Edifici C, Universitat Autònoma de Barcelona, 08193 Cerdanyola del Vallès, Spain.

Barts Cancer Institute, Queen Mary University of London, John Vane Science Centre, Charterhouse Square, London, United Kingdom.

出版信息

Bioorg Med Chem Lett. 2021 Apr 1;37:127840. doi: 10.1016/j.bmcl.2021.127840. Epub 2021 Feb 5.

Abstract

The transmetalation reaction between zinc dithiocarbamates functionalized with organic groups and the cation fac-[Tc(HO)(CO)] has been studied as a new strategy to bind biomolecules to this radionuclide for preparing radiopharmaceuticals with high molar activity. All complexes were obtained in high yields by heating at moderate temperatures and without subsequent purification. The chemical identity was ascertained by HPLC comparison with the homologous rhenium complexes. Stability studies in cysteine solution and serum have shown a good stability of the coordination set fac-[Tc(CO)(SS)(P)]. Preliminary biological studies of the radiocomplex functionalized with D-(+)-glucosamine with carcinoma cells have been performed.

摘要

锌二硫代氨基甲酸盐与有机基团的转金属反应已被研究为将生物分子与这种放射性核素结合的新策略,用于制备具有高摩尔活性的放射性药物。所有配合物均通过在中等温度下加热并随后不进行纯化而以高产率获得。通过与同系物铼配合物的 HPLC 比较确定了化学同一性。在半胱氨酸溶液和血清中的稳定性研究表明,[Tc(CO)(SS)(P)]配位基具有良好的稳定性。用 D-(+)-葡糖胺功能化的放射性配合物对癌细胞的初步生物学研究已经进行。

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