Abstract
A series of new 4-arylidene curcumin analogues (4-arylidene-1,7-bisarylhepta-1,6-diene-3,5-diones) were synthesized and found to be potent antiproliferative agents against a panel of cancer cell lines at submicromolar to low micromolar concentrations by SRB assay. Their inhibitory abilities against NF-κB was evaluated by High Content Analysis (HCA) based immunofluorescence assay; and the Akt signalling inhibition was determined by fluorescence polarization assay and western blot respectively. The Structure-Activity Relationship was discussed. Our results revealed that 4-arylidene curcumin analogues may work in a multi-targets manner in cancer cell.
Copyright © 2012 Elsevier Masson SAS. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / metabolism
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Chemistry Techniques, Synthetic
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Curcumin / chemical synthesis*
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Curcumin / chemistry
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Curcumin / metabolism
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Curcumin / pharmacology*
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Dose-Response Relationship, Drug
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Glycogen Synthase Kinase 3 / metabolism
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Glycogen Synthase Kinase 3 beta
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Humans
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Molecular Docking Simulation
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NF-kappa B / metabolism*
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Phosphorylation / drug effects
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Protein Conformation
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / metabolism
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Protein Kinase Inhibitors / pharmacology
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Protein Transport
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Proto-Oncogene Proteins c-akt / antagonists & inhibitors
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Proto-Oncogene Proteins c-akt / chemistry
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Proto-Oncogene Proteins c-akt / metabolism*
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Signal Transduction / drug effects*
Substances
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Antineoplastic Agents
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NF-kappa B
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Protein Kinase Inhibitors
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Glycogen Synthase Kinase 3 beta
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Proto-Oncogene Proteins c-akt
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Glycogen Synthase Kinase 3
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Curcumin