文献类型：期刊文献

英文题名：Design, synthesis and anti-GBM activities of amide-modified Curcumol derivatives

作者：Hu, Shiqi[1,2];Fan, Yuhang[1,2];Zhao, Yumo[1,2];Gao, Zhengyang[1,2];Lu, Jie[1,2];Li, Jian[1,2];Wei, Jinlian[1,2];Zhang, Yongqiang[1,2]

机构：[1]East China Univ Sci & Technol, Shanghai Frontiers Sci Ctr Optogenet Tech Cell Met, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China

年份：2025

卷号：125

外文期刊名：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:001495005700002)】；

基金：Financial support from the program of the National Natural Science Foundation of China (22171080, 22471072, Y.-Q. Z.) and Natural Science Foundation of Shanghai Municipality (23ZR1417200, Y.-Q. Z.) is gratefully acknowledged.

语种：英文

外文关键词：Curcumol; Amide-modification; Anti-GBM activity; BBB permeability

摘要：A series of amide-modified curcumol derivatives have been designed and synthesized via a simple four-step procedure. Notably, the derivatives with a phenyl or substituted phenyl attaching on the nitrogen atom showed significantly enhanced in vitro anti-GBM activity and excellent BBB permeability. Among them, 13t with a 4-fluorophenyl demonstrated the most potent dose-dependent inhibition of GBM cell viability, providing a novel lead compound for further anti-GBM drug discovery.