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An efficient and easily-accessible ligand for Cu(I)-catalyzed azide-alkyne cycloaddition bioconjugation.

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A novel ligand (6) for copper-catalyzed azide-alkyne cycloaddition (CuAAC) in bioconjugation has been developed. Both in vitro and in vivo experiments indicate that 6 is more efficient and less cytotoxic… Click to show full abstract

A novel ligand (6) for copper-catalyzed azide-alkyne cycloaddition (CuAAC) in bioconjugation has been developed. Both in vitro and in vivo experiments indicate that 6 is more efficient and less cytotoxic than the canonical CuAAC ligands. Besides, 6 is easily accessible and can be prepared at gram scale. Our study reveals that 6 might be an ideal CuAAC ligand for bioconjugations.

Keywords: easily accessible; alkyne cycloaddition; azide alkyne; catalyzed azide; ligand

Journal Title: Chemical communications
Year Published: 2020

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