Source:http://linkedlifedata.com/resource/pubmed/id/16953513
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
34
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pubmed:dateCreated |
2006-11-22
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pubmed:abstractText |
Pochonins A-F were recently characterized as six new members of the naturally occurring family of 14-membered resorcylic acid lactones. As there are a high number of ATPase and kinase inhibitors among natural resorcylic lactones, a library based on the pochonin scaffold, with five points of diversity, was prepared which includes diversity beyond that of the natural analogues. The library was synthesized by using solid-supported reagents amenable to automation. Testing the library for its inhibition against a panel of 24 kinases at 10 microM afforded a >14 % hit rate. These results demonstrate the potential of the resorcylides towards the inhibition of therapeutically relevant kinases.
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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/Adenosine Triphosphatases,
http://linkedlifedata.com/resource/pubmed/chemical/Enzyme Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Lactones,
http://linkedlifedata.com/resource/pubmed/chemical/Macrolides,
http://linkedlifedata.com/resource/pubmed/chemical/Phosphotransferases,
http://linkedlifedata.com/resource/pubmed/chemical/Resorcinols
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
0947-6539
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:day |
24
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
8819-34
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pubmed:dateRevised |
2009-8-4
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pubmed:meshHeading |
pubmed-meshheading:16953513-Adenosine Triphosphatases,
pubmed-meshheading:16953513-Drug Design,
pubmed-meshheading:16953513-Enzyme Inhibitors,
pubmed-meshheading:16953513-Lactones,
pubmed-meshheading:16953513-Macrolides,
pubmed-meshheading:16953513-Phosphotransferases,
pubmed-meshheading:16953513-Resorcinols,
pubmed-meshheading:16953513-Structure-Activity Relationship
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pubmed:year |
2006
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pubmed:articleTitle |
Diversity-oriented synthesis of pochonins and biological evaluation against a panel of kinases.
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pubmed:affiliation |
Organic and Bioorganic Chemistry Laboratory, Institut de Science et Ingénierie Supramoléculaires, Université Louis Pasteur-CNRS, 8 allée Gaspard Monge, 67000 Strasbourg, France.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Evaluation Studies
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