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

Yuan-Yang Guo; Bo Zhang; Luying Wang; Shenlong Huang; Shilei Wang; Yanbo You; Gongming Zhu; Anlian Zhu; Mingwei Geng; Lingjun Li

doi:10.1039/D0CC06348G

An efficient and easily-accessible ligand for Cu(i)-catalyzed azide–alkyne cycloaddition bioconjugation†

Yuan-Yang Guo,

‡^a Bo Zhang,‡^b Luying Wang,^a Shenlong Huang,^a Shilei Wang,^a Yanbo You,^a Gongming Zhu,^a Anlian Zhu,^a Mingwei Geng^a and Lingjun Li

*^a

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* Corresponding authors

^a School of Chemistry and Chemical engineering, Henan Normal University, Xinxiang 453007, China
E-mail: lingjunlee@htu.edu.cn

^b Department of Medical Research Center, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100730, China

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.

Chemical Communications

An efficient and easily-accessible ligand for Cu(i)-catalyzed azide–alkyne cycloaddition bioconjugation†

Abstract

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

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