Synthesis and biological evaluation of novel SIPI-7623 derivatives as farnesoid X receptor (FXR) antagonists

被引：0

作者：

Si-Yun Nian

Guo-Ping Wang

Zheng-Li Jiang

Ying Xiao

Mo-Han Huang

Yi-Huan Zhou

Xiang-Duan Tan

机构：

[1] Taizhou Hospital of Zhejiang Province,Department of Clinical Pharmacy

[2] China State Institute of Pharmaceutical Industry,Shanghai Institute of Pharmaceutical Industry

[3] Aurisco Pharmaceutical (Yangzhou) Co.,College of Pharmacy

[4] Ltd.,undefined

[5] Guilin Medical University,undefined

来源：

Molecular Diversity | 2019年 / 23卷

关键词：

FXR antagonists; Guggulsterone; Structure activity relationship; Molecular docking;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

Most of reported steroidal FXR antagonists are restricted due to low potency. We described the design and synthesis of novel nonsteroidal scaffold SIPI-7623 derivatives as FXR antagonists. The most potent compound A-11 (IC50 = 7.8 ± 1.1 μM) showed better activity compared to SIPI-7623 (IC50 = 40.8 ± 1.7 μM) and guggulsterone (IC50 = 45.9 ± 1.1 μM). Docking of A-11 in FXR’s ligand-binding domain was also studied.

引用

页码：19 / 33

页数：14

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