Source:http://linkedlifedata.com/resource/pubmed/id/19481464
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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
13
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pubmed:dateCreated |
2009-6-12
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pubmed:abstractText |
A series of novel 4-azaindolyl-indolyl-maleimides were synthesized and evaluated for their GSK-3beta inhibitory activity. Most compounds exhibited high potency to GSK-3beta. Among them, compound 7c was the most promising GSK-3beta inhibitor. Preliminary structure-activity relationships were discussed based on the experimental data obtained and showed that different substituents on the indole ring and side chains at 1-position of indole had varying degrees of influence on the GSK-3beta inhibitory potency. In a cell-based functional assay, compounds 7c and 15a significantly reduced Abeta-induced Tau hyperphosphorylation by inhibiting GSK-3beta.
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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 |
Jul
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
4302-12
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pubmed:dateRevised |
2011-11-2
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pubmed:meshHeading |
pubmed-meshheading:19481464-Cell Line, Tumor,
pubmed-meshheading:19481464-Glycogen Synthase Kinase 3,
pubmed-meshheading:19481464-Humans,
pubmed-meshheading:19481464-Maleimides,
pubmed-meshheading:19481464-Models, Molecular,
pubmed-meshheading:19481464-Neuroblastoma,
pubmed-meshheading:19481464-Phosphorylation,
pubmed-meshheading:19481464-Structure-Activity Relationship,
pubmed-meshheading:19481464-tau Proteins
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pubmed:year |
2009
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pubmed:articleTitle |
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.
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pubmed:affiliation |
ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
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pubmed:publicationType |
Journal Article
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