Synthesis and biological evaluation of novel SIPI-7623 derivatives as farnesoid X receptor (FXR) antagonists期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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

Authors:	Nian Si-Yun Wang Guo-Ping Jiang Zheng-Li Xiao Ying Huang Mo-Han Zhou Yi-Huan Tan Xiang-Duan

Institution:	1.Department of Clinical Pharmacy, Taizhou Hospital of Zhejiang Province, Xi Men Street No. 150, Linhai, 317000, Zhejiang Province, China ;2.Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Shanghai, 201203, China ;3.Aurisco Pharmaceutical (Yangzhou) Co., Ltd., Yangzhou, 225100, China ;4.College of Pharmacy, Guilin Medical University, Guilin, 541004, China ;

Abstract:	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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