Abstract
Structural modification of a compound discovered during screening using an HRE-dependent reporter assay has revealed a novel class of HIF-1 inhibitors, which potently inhibit the HIF-1alpha protein accumulation and its target gene expression under hypoxic conditions in human hepatocellular carcinoma Hep3B cells.
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 / pharmacology
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Aryl Hydrocarbon Receptor Nuclear Translocator / antagonists & inhibitors
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Benzoates / chemical synthesis*
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Benzoates / chemistry
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Benzoates / pharmacology
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Cell Hypoxia
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Cell Line, Tumor
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Erythropoietin / antagonists & inhibitors
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Erythropoietin / genetics
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Gene Expression
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Humans
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Hypoxia-Inducible Factor 1, alpha Subunit / antagonists & inhibitors*
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Hypoxia-Inducible Factor 1, alpha Subunit / biosynthesis
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RNA, Messenger / antagonists & inhibitors
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Structure-Activity Relationship
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Vascular Endothelial Growth Factor A / antagonists & inhibitors
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Vascular Endothelial Growth Factor A / genetics
Substances
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ARNT protein, human
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Antineoplastic Agents
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Benzoates
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HIF1A protein, human
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Hypoxia-Inducible Factor 1, alpha Subunit
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RNA, Messenger
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VEGFA protein, human
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Vascular Endothelial Growth Factor A
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Erythropoietin
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Aryl Hydrocarbon Receptor Nuclear Translocator