Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 13, Pages 3026-3029Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.05.024
Keywords
Kresoxim analogues; Cancer; Hypoxia-inducible factor-1 inhibitor; Mitochondrial respiration
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Funding
- Yeungnam University Research [216A251117]
- KRIBB Initiative of the Korea Research Council of Fundamental Science and Technology
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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.
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