Source:http://linkedlifedata.com/resource/pubmed/id/21273066
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2011-2-7
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pubmed:abstractText |
The synthesis of a small library of resorcylic acid lactones and evaluation of their biological properties as kinase inhibitors is described. Within the series E-enones were found more active than corresponding Z-enones as inhibitors of a subset of kinases containing a conserved cysteine. Replacement of the enone moiety with a ?-haloketone group led to compounds with an interesting kinase selectivity profile and also antiproliferative activity against Jurkat cells. An E-enone derivative also showed activity against capillary tube formation based on a co-culture of primary human umbilical cord endothelial cells (HUVECs) and vascular smooth muscle cells (vSMCs).
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Ketones,
http://linkedlifedata.com/resource/pubmed/chemical/Lactones,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Protein Kinases
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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 | |
pubmed:copyrightInfo |
Copyright © 2010 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 |
21
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1167-70
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pubmed:meshHeading |
pubmed-meshheading:21273066-Antineoplastic Agents,
pubmed-meshheading:21273066-Cells, Cultured,
pubmed-meshheading:21273066-Humans,
pubmed-meshheading:21273066-Isomerism,
pubmed-meshheading:21273066-Ketones,
pubmed-meshheading:21273066-Lactones,
pubmed-meshheading:21273066-Protein Kinase Inhibitors,
pubmed-meshheading:21273066-Protein Kinases,
pubmed-meshheading:21273066-Structure-Activity Relationship
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pubmed:year |
2011
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pubmed:articleTitle |
Isosteric replacement of the Z-enone with haloethyl ketone and E-enone in a resorcylic acid lactone series and biological evaluation.
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pubmed:affiliation |
School of Chemistry, National University of Ireland, Galway, University Road, Galway, Ireland.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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