論文

査読有り 最終著者 責任著者 国際誌
2019年8月

3H-Imidazo[4,5-b]pyridine-6-carboxylic acid derivatives as rexinoids with reduced teratogenicity

Bioorganic & Medicinal Chemistry Letters
  • Yuta Takamura
  • ,
  • Manami Takahashi
  • ,
  • Midori Nishii
  • ,
  • Osamu Shibahara
  • ,
  • Masaki Watanabe
  • ,
  • Michiko Fujihara
  • ,
  • Hiroki Kakuta

29
15
開始ページ
1891
終了ページ
1894
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/j.bmcl.2019.05.050
出版者・発行元
Elsevier {BV}

Several retinoid X receptor (RXR) ligands (rexinoids), such as bexarotene (1), exhibit teratogenicity, which is a serious impediment to their clinical application. We considered that rexinoids with a lower level of maximal RXR transcription activation (i.e., partial agonists) and lower lipid solubility might show weaker adverse side effects. Based on this idea, we modified our previously reported pentamethyltetralin-type RXR partial agonists 5 and 6 to reduce their lipophilicity. Here, we report a new RXR partial agonist, 3-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-2-(trifluoromethyl)-3H-imidazo[4,5-b]pyridine-6-carboxylic acid (8, CATF-PMN), which showed greatly reduced teratogenicity in zebrafish embryos.

リンク情報
DOI
https://doi.org/10.1016/j.bmcl.2019.05.050
PubMed
https://www.ncbi.nlm.nih.gov/pubmed/31160175
ID情報
  • DOI : 10.1016/j.bmcl.2019.05.050
  • ISSN : 0960-894X
  • ORCIDのPut Code : 58528054
  • PubMed ID : 31160175

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