期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 27, 期 13, 页码 3026-3029出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.05.024
关键词
Kresoxim analogues; Cancer; Hypoxia-inducible factor-1 inhibitor; Mitochondrial respiration
资金
- Yeungnam University Research [216A251117]
- KRIBB Initiative of the Korea Research Council of Fundamental Science and Technology
We designed and synthesized strobilurin analogues as hypoxia-inducible factor (HIF) inhibitors based on the molecular structure of kresoxim-methyl. Biological evaluation in human colorectal cancer HCT116 cells showed that most of the synthesized kresoxim-methyl analogues possessed moderate to potent inhibitory activity against hypoxia-induced HIF-1 transcriptional activation. Three candidates, compounds 11b, 11c, and 11d were identified as potent inhibitors against HIF-1 activation with IC50 values of 0.60-0.94 mu M. Under hypoxic condition, compounds 11b, 11c, and 11d increased the intracellular oxygen contents, thereby attenuating the hypoxia-induced accumulation of HIF-1 alpha protein. (C) 2017 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据