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

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

  • Bioorg Med Chem Lett. 2016 Dec 15;26(24):5887-5890. doi: 10.1016/j.bmcl.2016.11.009.
Shinichiro Fuse 1,  Toshiaki Ohuchi 1,  Yasunobu Asawa 1,  Shinichi Sato 1,  Hiroyuki Nakamura 2
Affiliations

Affiliations

  • 1 Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8503, Japan.
  • 2 Laboratory for Chemistry and Life Science, Institute of Innovative Research, Tokyo Institute of Technology, 4259 Nagatsuta-cho, Midori-ku, Yokohama 226-8503, Japan. Electronic address: hiro@res.titech.ac.jp.
PMID: 27847273 DOI: 10.1016/j.bmcl.2016.11.009
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/CH 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.

Keywords

CH direct arylation; Hypoxia inducible factor (HIF)-1; Imidazopyridine; Microwave.

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