NaClO-Mediated Cross Installation of Indoles and Azoles Benefits Anticancer Hit Discovery.

Changjun Yu, Ruiyao E, Xiao-Wei Zhang, Wen-Qian Hu, Guangjun Bao, Yiping Li, Yuyang Liu, Zeyuan He, Jingyue Li, Wen Ma, Ling-Yun Mou, Rui Wang, Wangsheng Sun

ChemMedChem 2023 Mar 01

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Innovations in synthetic chemistry have a profound impact on the drug discovery process, and will always be a necessary driver of drug development. As a result, it is of significance to develop novel simple and effective synthetic installation of medicinal modules to promote drug discovery. Herein, we have developed a NaClO-mediated cross installation of indoles and azoles, both of which are frequently encountered in drugs and natural products. This effective toolbox provides a convenient synthetic route to access a library of N-linked 2-(azol-1-yl) indole derivatives, and can be used for late-stage modification of drugs, natural products and peptides. Moreover, biological screening of the library has revealed that several adducts showed promising anticancer activities against A549 and NCI-H1975 cells, which give us a hit for anticancer drug discovery. © 2022 Wiley-VCH GmbH.

Citation

Changjun Yu, Ruiyao E, Xiao-Wei Zhang, Wen-Qian Hu, Guangjun Bao, Yiping Li, Yuyang Liu, Zeyuan He, Jingyue Li, Wen Ma, Ling-Yun Mou, Rui Wang, Wangsheng Sun. NaClO-Mediated Cross Installation of Indoles and Azoles Benefits Anticancer Hit Discovery. ChemMedChem. 2023 Mar 01;18(5):e202200651