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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2010-2-15
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pubmed:abstractText |
A series of boron-containing phenoxyacetanilide derivatives 8a-f, 9a-f, 15, and 16 were synthesized as hypoxia-inducible factor (HIF)-1alpha inhibitors. Among the compounds synthesized, carboranylphenoxyacetanilide 16 (GN26361) was found to be a potent inhibitor against HIF-1alpha accumulation under hypoxic conditions and inhibited the hypoxia-induced HIF-1 transcriptional activity in HeLa cells (IC50=0.74 microM). Compound 16 suppressed hypoxia-induced HIF-1alpha accumulation and vascular endothelial growth factor mRNA expression in a concentration-dependent manner without affecting the expression of HIF-1alpha mRNA.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:copyrightInfo |
Copyright 2009 Elsevier Ltd. All rights reserved.
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pubmed:issnType |
Electronic
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pubmed:day |
15
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pubmed:volume |
20
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1453-6
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pubmed:meshHeading |
pubmed-meshheading:20083404-Acetanilides,
pubmed-meshheading:20083404-Boron,
pubmed-meshheading:20083404-Boron Compounds,
pubmed-meshheading:20083404-Gene Expression Regulation,
pubmed-meshheading:20083404-HeLa Cells,
pubmed-meshheading:20083404-Humans,
pubmed-meshheading:20083404-Hypoxia-Inducible Factor 1, alpha Subunit,
pubmed-meshheading:20083404-Inhibitory Concentration 50,
pubmed-meshheading:20083404-Phenols,
pubmed-meshheading:20083404-RNA, Messenger,
pubmed-meshheading:20083404-Transcription, Genetic
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pubmed:year |
2010
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pubmed:articleTitle |
Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1alpha inhibitors.
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pubmed:affiliation |
Department of Chemistry, Faculty of Science, Gakushuin University, Mejiro, Tokyo 171-8588, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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