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rdf:type |
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|
lifeskim:mentions |
|
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pubmed:issue |
18
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pubmed:dateCreated |
2008-9-12
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pubmed:abstractText |
To characterize largazole's structural requirements for histone deacetylase (HDAC) inhibitory and antiproliferative activities, a series of analogues with modifications to the side chain or 16-membered macrocycle were prepared and biologically evaluated. Structure-activity relationships suggested that the four-atom linker between the macrocycle and octanoyl group in the side chain and the (S)-configuration at the C17 position are critical to repression of HDAC activity. However, the valine residue in the macrocycle can be replaced with alanine without significant loss of activity.
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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 |
Sep
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pubmed:issn |
1523-7052
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pubmed:author |
|
|
pubmed:issnType |
Electronic
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pubmed:day |
18
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pubmed:volume |
10
|
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4021-4
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
|
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pubmed:year |
2008
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pubmed:articleTitle |
Synthesis and activity of largazole analogues with linker and macrocycle modification.
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pubmed:affiliation |
Department of Chemistry, Duke University, Durham, North Carolina 27708, USA.
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|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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