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Title 

Synthesis and biological evaluation of kresoxim-methyl analogues as novel inhibitors of hypoxia-inducible factor (HIF)-1 accumulation in cancer cells

Authors 

S LeeOh Seok KwonChang-Soo LeeMi Sun WonHyun Seung BanC S Ra

Publisher 

Elsevier

Issue Date 

2017

Citation 

Bioorganic & Medicinal Chemistry Letters

Keywords 

CancerHypoxia-inducible factor-1 inhibitorKresoxim analoguesMitochondrial respiration

Abstract 

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??M. Under hypoxic condition, compounds 11b, 11c, and 11d increased the intracellular oxygen contents, thereby attenuating the hypoxia-induced accumulation of HIF-1α protein

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2017.05.024

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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