机构：[1]College of Chemical Engineering and Materials Science, Tianjin University of Science and Technology, Tianjin, 300457, China[2]Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, Shanghai, 201210, China[3]Institute of Drug Development & Chemical Biology, College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou, China[4]The Second Clinical Medical College, and Guangdong Provincial Key Laboratory of Clinical Research on Traditional Chinese Medicine Syndrome, Guangzhou University of Chinese Medicine, Guangzhou, China广东省中医院深圳市中医院深圳医学信息中心[5]Hangzhou Healsun Biopharm Co.,Ltd., China[6]Department of Orthopedics, Shanghai Key Laboratory of Orthopedics Implant, the Ninth People’s Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200011, China
Natural products play a key role in the history of human drug discovery, and especially for the anticancer agents. Copper(I)-catalyzed alkyne-azide [3+2] cycloaddition (CuAAC) reaction is perhaps the most powerful method for the efficient modification of complex natural products, enabling the direct incorporation of various functional groups accompanied by the formation of the multifunctional 1,2,3-triazole motif, which could not only serve as an basic and hydrophilic connecting group but also as a bioisosteres of 5-or 6-membered heterocycles or an amide group, thus facilitating the improvement of anticancer activities and/or drug-like properties. This contribution extensively summarizes the state-of-the-art application of 1,2,3-triazole in the modification of natural products for anticancer activity. The aim is to gain a deep understanding of the fruitful achievements as well as limitations of CuAAC click chemistry in natural product modification for anticancer activity, and provide perspectives and directions regarding future studies in natural product medicinal chemistry.
基金：
Natural Science Foundation of Zhejiang Province, China [LY22H300001]; Fundamental Research Funds for the Provincial Universities of Zhejiang, China [RF-A2022008]; National Natural Science Foundation of China [21977070, 21907085, U19A2011]
第一作者机构：[1]College of Chemical Engineering and Materials Science, Tianjin University of Science and Technology, Tianjin, 300457, China
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通讯作者：
推荐引用方式(GB/T 7714)：
Xiao Zaozao,Gu Yuang,Dong Hewei,et al.Strategic application of CuAAC click chemistry in the modification of natural products for anticancer activity[J].EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY REPORTS.2023,9:doi:10.1016/j.ejmcr.2023.100113.
APA：
Xiao, Zaozao,Gu, Yuang,Dong, Hewei,Liu, Bo,Jin, Weiwei...&Hou, Wei.(2023).Strategic application of CuAAC click chemistry in the modification of natural products for anticancer activity.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY REPORTS,9,
MLA：
Xiao, Zaozao,et al."Strategic application of CuAAC click chemistry in the modification of natural products for anticancer activity".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY REPORTS 9.(2023)
