Development of 1-aryl-3-furanyl/thienyl-imidazopyridine templates for inhibitors against hypoxia inducible factor (HIF)-1 transcriptional activity

Shinichiro Fuse, Toshiaki Ohuchi, Yasunobu Asawa, Shinichi Sato, Hiroyuki Nakamura

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)

Abstract

1,3-Disubstituted-imidazopyridines were designed for developing inhibitors against HIF-1 transcriptional activity. Designed compounds were rapidly synthesized from a key aromatic scaffold via microwave-assisted Suzuki-Miyaura coupling/C[sbnd]H direct arylation sequence. Evaluation of ability to inhibit the hypoxia induced transcriptional activity of HIF-1 revealed that the compound 2i and 3a retained the same level of the inhibitory activity comparing with that of known inhibitor, YC-1 (1). Identified, readily accessible 1-aryl-3-furanyl/thienyl-imidazopyridine templates should be useful for future drug development.

Original languageEnglish
Pages (from-to)5887-5890
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume26
Issue number24
DOIs
Publication statusPublished - 2016 Jan 1
Externally publishedYes

Keywords

  • C[sbnd]H direct arylation
  • Hypoxia inducible factor (HIF)-1
  • Imidazopyridine
  • Microwave

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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