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National Institute of Environmental Health Sciences

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Publication Detail

Title: Synthesis and biological evaluation of FICZ analogues as agonists of aryl hydrocarbon receptor.

Authors: Wu, Hao; Liu, Binkai; Yang, Ka; Winston-McPherson, Gabrielle N; Leisten, Eric D; Vezina, Chad M; Ricke, William A; Peterson, Richard E; Tang, Weiping

Published In Bioorg Med Chem Lett, (2020 Mar 01)

Abstract: 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.

PubMed ID: 31952965 Exiting the NIEHS site

MeSH Terms: Carbazoles/chemical synthesis; Carbazoles/pharmacology*; Cytochrome P-450 CYP1A1/metabolism; Dose-Response Relationship, Drug; Hep G2 Cells; Humans; Indoles/chemical synthesis; Indoles/pharmacology*; Molecular Structure; Receptors, Aryl Hydrocarbon/agonists*; Structure-Activity Relationship; Up-Regulation/drug effects

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