异恶唑
转录因子
缺氧诱导因子
报告基因
荧光素酶
化学
IC50型
癌症研究
抄写(语言学)
缺氧诱导因子1
缺氧(环境)
分子生物学
生物
基因
体外
生物化学
转染
立体化学
基因表达
氧气
哲学
有机化学
语言学
作者
Zian Xue,Huiti Li,Wei Xie,Ying Xu,Lu Zhou,Zhi-bei Qu
标识
DOI:10.1021/acsmedchemlett.2c00308
摘要
Hypoxia-inducible factor, also known as HIF, is a transcriptional factor universally found in mammalian cells. HIF-1 is one of the HIF-families and acts as a heterodimer consisting of α and β subunits. It is found to play significant roles in pathologic conditions such as tumor development and metastasis. Here, we first report benzo[d]isoxazole analogues as HIF-1α transcription inhibitors. Thereby, we designed and synthesized 26 benzo[d]isoxazole derivatives and evaluated their inhibitory activities against HIF-1α transcription in HEK293T cells by a dual-luciferase gene reporter assay. Among them, compounds 15 and 31 showed the best efficacy in a cell-based assay with an IC50 value of 24 nM and have potential antitumor effects for further development.
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