Foxo3a Inhibitors of Microbial Origin, JBIR-141 and JBIR-142

Teppei Kawahara, Noritaka Kagaya, Yuichi Masuda, Takayuki Doi, Miho Izumikawa, Kumiko Ohta, Atsushi Hirao, Kazuo Shin-Ya

研究成果: Article査読

3 被引用数 (Scopus)

抄録

JBIR-141 (1) and JBIR-142 (2) were discovered as potent Foxo3a inhibitors that consist of three quite unique substructures, a 1-((dimethylamino)ethyl)-5-methyl-4,5-dihydrooxazole-4-carboxylic acid that is originated from Ala-Thr amino acid residues, a 3-acetoxy-4-amino-7-(hydroxy(nitroso)amino)-2,2-dimethylheptanoic acid, and an α-acyl tetramic acid fused with a 2-methylpropan-1-ol moiety. Their structures involving absolute configurations were determined by spectroscopic data, chemical degradation, anisotropy methods, and LC-MS analyses of diastereomeric derivatives. Compounds 1 and 2 exhibited specific inhibition against Foxo3a transcriptional activity with IC50 values of 23.1 and 166.2 nM, respectively.

本文言語English
ページ(範囲)5476-5479
ページ数4
ジャーナルOrganic letters
17
21
DOI
出版ステータスPublished - 2015 11 6

ASJC Scopus subject areas

  • 生化学
  • 物理化学および理論化学
  • 有機化学

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