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Click chemistry is perhaps the most powerful synthetic toolbox that can efficiently access the molecular diversity and unique functions of complex natural products up to now. It enables the ready synthesis of diverse sets of natural product derivatives either for the optimization of their drawbacks or for the construction of natural product-like drug screening libraries. This paper showcases the state-of-the-art development of click chemistry in natural product modification and summarizes thedoi:10.3389/fchem.2021.774977 pmid:34869223 pmcid:PMC8635925 fatcat:trkkqm2tyzd2de4325s6fy37oe