HBED-NN: a bifunctional chelator for constructing radiopharmaceuticals

Radiometal-based radiopharmaceuticals bearing bifunctional HBED chelators are powerful radiotracers for cancer diagnosis and therapy. Bifunctional HBED chelators make strong complexes with trivalent gallium and are able to bind to bioactive molecules through covalent bonds. However, thus far, no bif...

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Hauptverfasser: Makarem, Ata (VerfasserIn) , Klika, Karel D. (VerfasserIn) , Litau, German (VerfasserIn) , Remde, Yvonne (VerfasserIn) , Kopka, Klaus (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: May 8, 2019
In: The journal of organic chemistry
Year: 2019, Jahrgang: 84, Heft: 11, Pages: 7501-7508
ISSN:1520-6904
DOI:10.1021/acs.joc.9b00832
Online-Zugang:Verlag, Volltext: https://doi.org/10.1021/acs.joc.9b00832
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Verfasserangaben:Ata Makarem, Karel D. Klika, German Litau, Yvonne Remde, and Klaus Kopka

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520 |a Radiometal-based radiopharmaceuticals bearing bifunctional HBED chelators are powerful radiotracers for cancer diagnosis and therapy. Bifunctional HBED chelators make strong complexes with trivalent gallium and are able to bind to bioactive molecules through covalent bonds. However, thus far, no bifunctional HBED chelator capable of direct conjugation via click chemistry has been reported. We hereby introduce HBED-NN as a structurally new bifunctional HBED chelator for direct click coupling. We also investigated the complex chemistry of [Ga-(HBED-NN)] for potential use in gallium-based radiopharmaceuticals. 
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