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

研究成果: Article査読

18 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)5887-5890
ページ数4
ジャーナルBioorganic and Medicinal Chemistry Letters
26
24
DOI
出版ステータスPublished - 2016
外部発表はい

ASJC Scopus subject areas

  • 生化学
  • 分子医療
  • 分子生物学
  • 薬科学
  • 創薬
  • 臨床生化学
  • 有機化学

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