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. 2023 Mar 1;18(5):e202200651.
doi: 10.1002/cmdc.202200651. Epub 2023 Jan 18.

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

Changjun Yu  1 , Ruiyao E  1 , Xiao-Wei Zhang  1 , Wen-Qian Hu  1 , Guangjun Bao  1 , Yiping Li  1 , Yuyang Liu  1 , Zeyuan He  1 , Jingyue Li  1 , Wen Ma  1 , Ling-Yun Mou  1 , Rui Wang  1   2 , Wangsheng Sun  1
Affiliations

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

Changjun Yu et al. ChemMedChem. .

Abstract

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.

Keywords: anticancer; azoles; cross installation; indoles.

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