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rdf:type |
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lifeskim:mentions |
umls-concept:C0014442,
umls-concept:C0026381,
umls-concept:C0028131,
umls-concept:C0030015,
umls-concept:C0079411,
umls-concept:C0439284,
umls-concept:C0441655,
umls-concept:C0443286,
umls-concept:C0456387,
umls-concept:C0598128,
umls-concept:C1140150,
umls-concept:C1333895,
umls-concept:C1512474,
umls-concept:C1524063,
umls-concept:C2266853
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pubmed:issue |
15
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pubmed:dateCreated |
2008-8-7
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|
pubmed:abstractText |
A series of hydroxamate based HDAC inhibitors containing a phenylisoxazole as the CAP group has been synthesized using nitrile oxide cycloaddition chemistry. An HDAC6 selective inhibitor having a potency of approximately 2 picomolar was identified. Some of the compounds were examined for their ability to block pancreatic cancer cell growth and found to be about 10-fold more potent than SAHA. This research provides valuable, new molecular probes for use in exploring HDAC biology.
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pubmed:grant |
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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 |
Aug
|
|
pubmed:issn |
1520-4804
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|
pubmed:author |
|
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pubmed:issnType |
Electronic
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pubmed:day |
14
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pubmed:volume |
51
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4370-3
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pubmed:dateRevised |
2010-12-3
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pubmed:meshHeading |
pubmed-meshheading:18642892-Binding Sites,
pubmed-meshheading:18642892-Cell Line, Tumor,
pubmed-meshheading:18642892-Cell Proliferation,
pubmed-meshheading:18642892-Enzyme Inhibitors,
pubmed-meshheading:18642892-Histone Deacetylase Inhibitors,
pubmed-meshheading:18642892-Histone Deacetylases,
pubmed-meshheading:18642892-Humans,
pubmed-meshheading:18642892-Models, Molecular,
pubmed-meshheading:18642892-Molecular Probes,
pubmed-meshheading:18642892-Molecular Structure,
pubmed-meshheading:18642892-Nitriles,
pubmed-meshheading:18642892-Oxides,
pubmed-meshheading:18642892-Structure-Activity Relationship
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pubmed:year |
2008
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pubmed:articleTitle |
Use of the nitrile oxide cycloaddition (NOC) reaction for molecular probe generation: a new class of enzyme selective histone deacetylase inhibitors (HDACIs) showing picomolar activity at HDAC6.
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pubmed:affiliation |
Department of Medicinal Chemistry & Pharmacognosy, Drug Discovery Program, University of Illinois at Chicago, 833 South Wood Street, Chicago, Illinois 60612, USA. Kozikowa@uic.edu
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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