European Journal of Medicinal Chemistry p. 303 - 309 (2017)
Update date:2022-07-30
Topics:
Zhang, Guoning
Liu, Shuainan
Tan, Wenjuan
Verma, Ruchi
Chen, Yuan
Sun, Deyang
Huan, Yi
Jiang, Qian
Wang, Xing
Wang, Na
Xu, Yang
Wong, Chiwai
Shen, Zhufang
Deng, Ruitang
Liu, Jinsong
Zhang, Yanqiao
Fang, Weishuo
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.
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