期刊
JOURNAL OF ORGANOMETALLIC CHEMISTRY
卷 798, 期 -, 页码 189-195出版社
ELSEVIER SCIENCE SA
DOI: 10.1016/j.jorganchem.2015.05.029
关键词
meta-Carborane; Hypoxia inducible factor; Transcription; Inhibitor
资金
- Ministry of Education, Culture, Sports, Science and Technology, Japan [26102721]
- Grants-in-Aid for Scientific Research [26102721] Funding Source: KAKEN
meta-Carboranylphenoxyacetanilides were synthesized by copper catalyzed coupling reaction of meta-carborane and phenyl iodides. The synthesized compounds were evaluated for their ability to inhibit hypoxia-induced HIF-1 transcriptional activity using a cell-based reporter gene assay. Among the compounds synthesized, meta-carborane containing phenoxyanilides 2d and 2h, which have an isobutyl group on meta-carborane, exhibited significant inhibition of hypoxia-induced HIF-1 transcriptional activity toward HeLa cell-based reporter gene assay with the IC50 values of 0.73 and 0.55 mu M, respectively. (C) 2015 Elsevier B.V. All rights reserved.
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