Abstract
A series of oxazolidinone and indole derivatives were synthesized and evaluated as IL-6 signaling blockers by measuring the effects of these compounds on IL-6-induced luciferase expression in human hepatocarcinoma HepG2 cells transfected with p-STAT3-Luc. Among different compounds screened, compound 4d was emerged as the most potent IL-6 signaling blockers with IC50 value of 5.9 μM which was much better than (+)-Madindoline A (IC50=21 μM), a known inhibitor of IL-6.
Keywords:
IL-6 antagonists; IL-6 signaling inhibitor; Oxazolidinone; Rheumatoid arthritis; STAT3; gp130.
Copyright © 2016 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Binding Sites
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Bridged Bicyclo Compounds, Heterocyclic / chemistry
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Crystallography, X-Ray
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Hep G2 Cells
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Humans
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Indoles / chemistry
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Inhibitory Concentration 50
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Interleukin-6 / antagonists & inhibitors
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Interleukin-6 / metabolism*
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Molecular Docking Simulation
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Oxazolidinones / chemical synthesis
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Oxazolidinones / chemistry*
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Oxazolidinones / pharmacology
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Protein Structure, Tertiary
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STAT3 Transcription Factor / genetics
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STAT3 Transcription Factor / metabolism
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Signal Transduction / drug effects*
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Structure-Activity Relationship
Substances
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Bridged Bicyclo Compounds, Heterocyclic
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Indoles
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Interleukin-6
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Oxazolidinones
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STAT3 Transcription Factor
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madindoline A