Synthesis and Evaluation of Celastrol Derivatives as HIF-1α Inhibitors

被引：0
|
作者：
Xiaoqun Ren
Linlin Cui
Yang Wang
Huayun Li
Guanghuan Shen
机构：
[1] The Affiliated Hospital of Southwest Medical University,College of Pharmacy
[2] Harbin University of Commerce,undefined
来源：
Chemistry of Natural Compounds | 2022年 / 58卷
关键词：
HIF-1α; celastrol; cytotoxicity; Hep3B cells;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A series of celastrol derivatives were synthesized and evaluated as hypoxia-inducible factor-1α (HIF-1α) inhibitors. Among these compounds, 4b and 4d appeared to have high HIF-1α inhibitory activity of 2.97 and 2.99 μM IC50 values respectively. The cytotoxicity of these compounds was also assessed in Hep3B cells using the MTT assay, and no compounds showed any appreciable cytotoxic activity (IC50 > 50 μmol/L).
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页码：1075 / 1078
页数：3
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