Source:http://linkedlifedata.com/resource/pubmed/id/15362121
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
9
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pubmed:dateCreated |
2004-9-13
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pubmed:abstractText |
Multiple linear regression analysis was employed in an effort to establish a quantitative structure-activity relationship model for the CDK1-inhibitory activity of a series of 9-substituted paullones. While the electronic properties of the 9-substituents proved to be of high relevance for CDK1 inhibition, both lipophilic and a steric parameters could not be included in a meaningful equation for the calculation of biological properties. The equation solely based on the electronic parameter was successfully used for the prediction of the CDK1-inhibitory activity of a small test set comprising novel paullones with sulfur-containing 9-substituents. Among these new derivatives, 2-methoxy-9-methylsulfonylpaullone proved to be superior to the standard alsterpaullone with respect to CDK1 inhibition.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Sep
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pubmed:issn |
0365-6233
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
337
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
486-92
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:15362121-Animals,
pubmed-meshheading:15362121-Benzazepines,
pubmed-meshheading:15362121-CDC2 Protein Kinase,
pubmed-meshheading:15362121-Electrons,
pubmed-meshheading:15362121-Enzyme Inhibitors,
pubmed-meshheading:15362121-Indoles,
pubmed-meshheading:15362121-Linear Models,
pubmed-meshheading:15362121-Molecular Structure,
pubmed-meshheading:15362121-Quantitative Structure-Activity Relationship,
pubmed-meshheading:15362121-Starfish
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pubmed:year |
2004
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pubmed:articleTitle |
CDK1-inhibitory activity of paullones depends on electronic properties of 9-substituents.
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pubmed:affiliation |
Universität Hamburg, Institut für Pharmazie, Hamburg, Germany.
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pubmed:publicationType |
Journal Article
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