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.
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页码：19 / 33
页数：14
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