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HIF-1 alpha inhibitors: Synthesis and biological evaluation of novel moracin O and P analogues

Authors
Xia, YanJin, YinglanKaur, NavneetChoi, YongseokLee, 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
URI
https://scholar.korea.ac.kr/handle/2021.sw.korea/112274
DOI
10.1016/j.ejmech.2011.03.022
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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생명과학대학 (생명공학부)
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