1393580-83-0Relevant articles and documents
Discovery and optimization of 1,3,4-trisubstituted-pyrazolone derivatives as novel, potent, and nonsteroidal farnesoid X receptor (FXR) selective antagonists
Huang, Huang,Yu, Ying,Gao, Zhenting,Jin, Hui,Yan, Wenzhong,Ma, Ruoqun,Zhu, Jin,Shen, Xu,Jiang, Hualiang,Li, Jian,Li, Chenjing,Xu, Xing,Chen, Lili,Zhang, Yong
, p. 7037 - 7053,17 (2012/12/11)
LBVS of 12480 in-house compounds, followed by HTRF assay, resulted in one nonsteroidal compound (11) with antagonistic activity against FXR (69.01 ± 11.75 μM). On the basis of 11, 26 new derivatives (12a-z) were designed and synthesized accordingly. Five