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

40 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 1

Fingerprint

Hypoxia-Inducible Factor 1
Structure-Activity Relationship
Biological Products
Gene expression
Scaffolds
Tumors
Cells
Gene Expression
Neoplasms
Proteins
moracin P
moracin O
Tumor Hypoxia
benzofuran
In Vitro Techniques
Hypoxia

Keywords

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

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Pharmacology

Cite this

HIF-1α inhibitors : Synthesis and biological evaluation of novel moracin O and P analogues. / Xia, Yan; Jin, Yinglan; Kaur, Navneet; Choi, Yongseok; Lee, Kyeong.

In: European Journal of Medicinal Chemistry, Vol. 46, No. 6, 01.06.2011, p. 2386-2396.

Research output: Contribution to journalArticle

Xia, Yan ; Jin, Yinglan ; Kaur, Navneet ; Choi, Yongseok ; Lee, Kyeong. / HIF-1α inhibitors : Synthesis and biological evaluation of novel moracin O and P analogues. In: European Journal of Medicinal Chemistry. 2011 ; Vol. 46, No. 6. pp. 2386-2396.
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