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

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A Multifunctional HBED-Type Chelator with Dual Conjugation Capabilities for Radiopharmaceutical Development
Synlett ( IF 1.7 ) Pub Date : 2019-08-26 , DOI: 10.1055/s-0039-1690194
Ata Makarem _{1,

2} , Mohammadreza Kamali Sarvestani _{1,

3} , Karel D. Klika ₄ , Klaus Kopka _{1,

5}

Affiliation

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.

中文翻译：

用于放射性药物开发的具有双重偶联能力的多功能 HBED 型螯合剂

双功能 HBED 螯合剂是六齿络合配体（螯合剂），与三价镓紧密配合，此外，还能够与生物活性分子结合。在核医学中，基于 HBED 的放射性药物被用作强大的放射性示踪剂，用于肿瘤成像。在双功能 HBED 螯合剂的变体中，HBED-CC 是最著名的。它具有两个末端羧酸基团，能够通过形成酰胺键进行生物共轭。然而，为了允许通过点击耦合进行生物共轭，我们之前修改了 HBED-CC 的结构并引入了带有两个叠氮化物功能的 HBED-NN 螯合剂。我们现在将 HBED-CC 和 HBED-NN 螯合剂的共轭能力结合在一个分子中，并创造了 HBED-NC，它同时具有叠氮化物和羧酸基团。HBED-NC 的优势在于它为构建单体或异二聚体放射性标记前体提供了选择。这项工作描述了通过两种途径之一合成 HBED-NC。

更新日期：2019-08-26

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