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

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• 作者：Shinichiro Fuse ; Toshiaki Ohuchi ; Yasunobu Asawa ; Shinichi Sato ; Hiroyuki Nakamura ; ^{hiro@res.titech.ac.jp}
• 关键词：Hypoxia inducible factor (HIF)-1 ; Imidazopyridine ; CH direct arylation ; Microwave
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 December 2016
• 年：2016
• 卷：26
• 期：24
• 页码：5887-5890
• 全文大小：691 K
• 卷排序：26

文摘

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.