Abstract
The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.
Original language | English |
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Pages (from-to) | 2386-2396 |
Number of pages | 11 |
Journal | European Journal of Medicinal Chemistry |
Volume | 46 |
Issue number | 6 |
DOIs | |
State | Published - Jun 2011 |
Keywords
- Arylbenzofuran
- HIF-1α
- Moracin
- Structure-activity relationships