Discovery and SAR study of hydroxyacetophenone derivatives as potent, non-steroidal farnesoid X receptor (FXR) antagonists

P Liu, X Xu, L Chen, L Ma, X Shen, L Hu

文献索引：Liu, Peng; Xu, Xing; Chen, Lili; Ma, Lei; Shen, Xu; Hu, Lihong Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 5 p. 1596 - 1607

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被引用次数: 8

摘要

Abstract Compound 1 (IC 50= 35.2±7.2 μM), a moderate FXR antagonist was discovered via high-throughput screening. Structure–activity relationship studies indicated that the shape and the lipophilicity of the substituents of the aromatic ring affect the activity dramatically, increasing the shape and the lipophilicity of the substituents of the aromatic ring enhances the potency of FXR antagonists. Especially, when the OH at C2 position of the aromatic ...