| Literature DB >> 28235703 |
Guoning Zhang1, Shuainan Liu1, Wenjuan Tan2, Ruchi Verma3, Yuan Chen3, Deyang Sun1, Yi Huan1, Qian Jiang1, Xing Wang1, Na Wang4, Yang Xu5, Chiwai Wong2, Zhufang Shen1, Ruitang Deng3, Jinsong Liu4, Yanqiao Zhang5, Weishuo Fang6.
Abstract
Farnesoid X receptor (FXR), a nuclear receptor mainly distributed in liver and intestine, has been regarded as a potential target for the treatment of various metabolic diseases, cancer and infectious diseases related to liver. Starting from two previously identified chalcone-based FXR antagonists, we tried to increase the activity through the design and synthesis of a library containing chalcones, flavones and chromenes, based on substitution manipulation and conformation (ring closure) restriction strategy. Many chalcones and four chromenes were identified as microM potent FXR antagonists, among which chromene 11c significantly decreased the plasma and hepatic triglyceride level in KKay mice.Entities:
Keywords: Antagonist; Chalcones; Chromenes; Farnesoid X receptor
Mesh：
Substances：
Year: 2017 PMID： 28235703 PMCID： PMC5505628 DOI： 10.1016/j.ejmech.2017.02.037
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514