Copper Catalysis in Living Systems and In Situ Drug Synthesis. (15th November 2016)

• Record Type: Journal Article
• Authors: Clavadetscher, Jessica; Hoffmann, Scott; Lilienkampf, Annamaria; Mackay, Logan; Yusop, Rahimi M.; Rider, Sebastien A.; Mullins, John J.; Bradley, Mark
• Is Part Of: Angewandte Chemie. Volume 128:Number 50(2016)
• Page Start: 15891
• Page End: 15895
• Publication Date: 2016-11-15
• Subjects: Bioorthogonale Chemie -- Heterogene Katalyse -- Kupfer -- Prodrugs; Chemistry -- Periodicals; 540
• DOI: 10.1002/ange.201609837
• Languages: English
• ISSNs: 0044-8249

Abstract

Abstract: 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 in vivo 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 in situ generation of a triazole‐containing anticancer agent from two benign components, opening up many new avenues of exploration for CuAAC chemistry.