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rdf:type |
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lifeskim:mentions |
umls-concept:C0205314,
umls-concept:C0220781,
umls-concept:C0679622,
umls-concept:C1167622,
umls-concept:C1512474,
umls-concept:C1513371,
umls-concept:C1524081,
umls-concept:C1707689,
umls-concept:C1883254,
umls-concept:C2266853,
umls-concept:C2603343
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pubmed:issue |
24
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pubmed:dateCreated |
2003-12-3
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pubmed:abstractText |
In order to find novel non-hydroxamate histone deacetylase (HDAC) inhibitors, a series of compounds modeled after suberoylanilide hydroxamic acid (SAHA) were designed and synthesized as (i). substrate (acetyl lysine) analogues (compounds 3-7), (ii). analogues bearing various functional groups expected to chelate zinc ion (compounds 8-15), and (iii). analogues bearing nucleophilic functional groups which could bind covalently to HDACs (compounds 16-18). In this series, semicarbazide 8b and bromoacetamides 18b,c were found to be potent HDAC inhibitors for non-hydroxamates.
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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 |
Dec
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pubmed:issn |
0960-894X
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pubmed:author |
|
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
13
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4321-6
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:14643318-Binding Sites,
pubmed-meshheading:14643318-Drug Design,
pubmed-meshheading:14643318-Enzyme Inhibitors,
pubmed-meshheading:14643318-Histone Deacetylase Inhibitors,
pubmed-meshheading:14643318-Histone Deacetylases,
pubmed-meshheading:14643318-Hydroxamic Acids,
pubmed-meshheading:14643318-Indicators and Reagents,
pubmed-meshheading:14643318-Lysine,
pubmed-meshheading:14643318-Models, Molecular,
pubmed-meshheading:14643318-Molecular Conformation,
pubmed-meshheading:14643318-Protein Conformation,
pubmed-meshheading:14643318-Structure-Activity Relationship
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pubmed:year |
2003
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pubmed:articleTitle |
Novel histone deacetylase inhibitors: design, synthesis, enzyme inhibition, and binding mode study of SAHA-based non-hydroxamates.
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pubmed:affiliation |
Graduate School of Pharmaceutical Sciences, Nagoya City University, 3-1 Tanabe-dori, Mizuho-ku, Nagoya, Aichi 467-8603, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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