文献类型：期刊文献

英文题名：Design and synthesis of indol-2-one derivatives as potential RET inhibitors

作者：Li, Zhenzhu[1];Sun, Kai[2,3];Xu, Yuanhong[1];Zhu, Fuli[1];Mao, Zhenyu[1];Wang, Yang[2,3];Yuan, Yaxia[4];Qiu, Ting[1,2,3];Chen, Xiabin[1,2,3];Ma, Lei[1]

机构：[1]East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, 130 Meilong Rd, Shanghai 200237, Peoples R China;[2]Hangzhou Normal Univ, Sch Pharm, Hangzhou 311121, Zhejiang, Peoples R China;[3]Hangzhou Normal Univ, Collaborat Innovat Ctr Tradit Chinese Med Zhejiang, Key Lab Elemene Class Anticanc Chinese Med, Engn Lab Dev & Applicat Tradit Chinese Med, Hangzhou 311121, Zhejiang, Peoples R China;[4]Univ Texas Hlth Sci Ctr San Antonio, Dept Biochem & Struct Biol, San Antonio, TX 78229 USA

年份：2024

卷号：97

外文期刊名：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001164573500001)】；

基金：This work was supported by the National Natural Science Foundation of China (Grants 82373739, 81973196) .

语种：英文

外文关键词：RET kinase inhibitors; Indol-2-one; Structure-based optimization; Cell proliferation; Structure-activity relationship

摘要：We synthesized and assessed five series of indol-2-one derivatives for their potential as RET kinase inhibitors. Notably, compounds B3, B6, D1, D2, D3, and D5 demonstrated significant inhibitory activity. Among these, D5 exhibited the best activity of inhibiting RET kinase, which provided reference for the subsequent development of RET kinase inhibitors as anti-thyroid cancer chemical.