Copper Catalysis in Living Systems and InSitu Drug Synthesis

The copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction has proven to be a pivotal advance in chemical ligation strategies with applications ranging from polymer fabrication to bioconjugation. However, application invivo has been limited by the inherent toxicity of the copper catalyst. Here...

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Published inAngewandte Chemie International Edition Vol. 55; no. 50; p. 15662
Main Authors Clavadetscher, Jessica, Hoffmann, Scott, Lilienkampf, Annamaria, Mackay, Logan, Yusop, Rahimi M, Rider, Sebastien A, Mullins, John J, Bradley, Mark
Format Journal Article
LanguageEnglish
Published Weinheim Wiley Subscription Services, Inc 12.12.2016
EditionInternational ed. in English
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Summary:The copper-catalyzed azide-alkyne cycloaddition (CuAAC) reaction has proven to be a pivotal advance in chemical ligation strategies with applications ranging from polymer fabrication to bioconjugation. However, application invivo has been limited by the inherent toxicity of the copper catalyst. Herein, we report the application of heterogeneous copper catalysts in azide-alkyne cycloaddition processes in biological systems ranging from cells to zebrafish, with reactions spanning from fluorophore activation to the first reported insitu generation of a triazole-containing anticancer agent from two benign components, opening up many new avenues of exploration for CuAAC chemistry.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201609837