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Synthesis and biological evaluation of FICZ analogues as agonists of aryl hydrocarbon receptor.
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2020-01-07 , DOI: 10.1016/j.bmcl.2020.126959
Hao Wu 1 , Binkai Liu 1 , Ka Yang 1 , Gabrielle N Winston-McPherson 1 , Eric D Leisten 1 , Chad M Vezina 2 , William A Ricke 3 , Richard E Peterson 1 , Weiping Tang 4
Affiliation  

The aryl hydrocarbon receptor (AhR) is a ligand activated transcription factor involved in multiple biological processes including immune cell differentiation, intestinal function and inflammation. Based on the scaffold of naturally occurring AhR ligand 6-formylindolo (3,2-b) carbazole (FICZ, 2), a series of analogues has been designed, synthesized and evaluated by cell-based assays. The structure-activity relationships study has successfully led to the discovery of compound 11e with extremely potent activity.

中文翻译:

作为芳烃受体激动剂的 FICZ 类似物的合成和生物学评价。

芳烃受体(AhR)是一种配体激活的转录因子,参与多种生物过程,包括免疫细胞分化、肠道功能和炎症。基于天然存在的 AhR 配体 6-甲酰基吲哚 (3,2-b) 咔唑 (FICZ, 2) 的支架,一系列类似物已被设计、合成并通过基于细胞的测定进行评估。构效关系研究成功发现了具有极强活性的化合物11e。
更新日期:2020-01-07
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