2019年8月
3H-Imidazo[4,5-b]pyridine-6-carboxylic acid derivatives as rexinoids with reduced teratogenicity
Bioorganic & Medicinal Chemistry Letters
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- 巻
- 29
- 号
- 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
- ID情報
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- DOI : 10.1016/j.bmcl.2019.05.050
- ISSN : 0960-894X
- ORCIDのPut Code : 58528054
- PubMed ID : 31160175