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HIF-1 alpha inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues
- Authors
- Xia, Yan; Jin, Yinglan; Kaur, Navneet; Choi, Yongseok; Lee, Kyeong
- Issue Date
- 6월-2011
- Publisher
- ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
- Keywords
- Moracin; Arylbenzofuran; HIF-1 alpha; Structure-activity relationships
- Citation
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.46, no.6, pp.2386 - 2396
- Indexed
- SCIE
SCOPUS
- Journal Title
- EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
- Volume
- 46
- Number
- 6
- Start Page
- 2386
- End Page
- 2396
- ISSN
- 0223-5234
- 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-1 alpha protein accumulation and target gene expression under hypoxia. (C) 2011 Elsevier Masson SAS. All rights reserved.
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