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A Multifunctional HBED-Type Chelator with Dual Conjugation Capabilities for Radiopharmaceutical Development

机译:一种多功能HBED型螯合剂,具有用于放射性药物开发的双缀合能力

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摘要

Bifunctional HBED chelators are hexadentate complexing ligands (chelators) that tightly coordinate to trivalent gallium and, additionally, are able to bind to bioactive molecules. In nuclear medicine, HBED-based radiopharmaceuticals are used as powerful radiotracers for tumor imaging. Among variants of bifunctional HBED chelators, HBED-CC is the most well-known; it possesses two terminal carboxylic acid groups that are able to undergo bioconjugation by amide-bond formation. However, to permit bioconjugation through click coupling, we previously modified the structure of HBED-CC and introduced HBED-NN chelator bearing two azide functions. We have now combined the conjugation capabilities of HBED-CC and HBED-NN chelators in one molecule and have created HBED-NC, which possesses both azide and carboxylic acid groups. The advantage of HBED-NC is that it provides options for constructing either monomeric or heterodimeric radiolabeling precursors. This work describes the synthesis of HBED-NC by either of two pathways.
机译:双官能HBBED螯合剂是六种络合配体(螯合剂),其紧紧地与三价镓坐标,并且另外,能够与生物活性分子结合。在核医学中,基于HBED的放射性药物用作肿瘤成像的强大反脱机。在双官能HBBED螯合剂的变体中,HBED-CC是最着名的;它具有两个末端羧酸基团,其能够通过酰胺键形成进行生物缀合。然而,为了通过点击耦合允许生物谐波,我们之前修改了HBED-CC的结构并引入了轴承两个叠氮化器功能的HBED-NN螯合剂。我们现在已经在一个分子中组合了HBED-CC和HBED-NN螯合剂的共轭能力并产生了HBED-NC,其具有叠氮和羧酸基团。 HBED-NC的优点是它提供了构建单体或异二聚体放射性标记前体的选择。这项工作描述了两种途径中的任何一种合成HBED-NC。

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