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

Yan Xia, Yinglan Jin, Navneet Kaur, Yongseok Choi, Kyeong Lee

Research output: Contribution to journalArticle

44 Citations (Scopus)

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 languageEnglish
Pages (from-to)2386-2396
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume46
Issue number6
DOIs
Publication statusPublished - 2011 Jun

Keywords

  • Arylbenzofuran
  • HIF-1α
  • Moracin
  • Structure-activity relationships

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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