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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
2008-1-9
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pubmed:abstractText |
A series of indenopyrazoles 8 and 9 were designed and synthesized as EGFR tyrosine kinase inhibitors by in silico high-throughput screening. Compounds 8b and 8d showed significant inhibition of A431 cell growth (GI50 = 0.062 and 0.057 microM, respectively). Compounds 8b and 9a showed inhibitory activity toward both EGFR and VEGFR-2 (KDR) tyrosine kinases, whereas 8d inhibited VEGFR-2 tyrosine kinase, exclusively.
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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 |
Jan
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pubmed:issn |
1464-3405
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
285-8
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pubmed:dateRevised |
2009-11-19
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pubmed:meshHeading |
pubmed-meshheading:17983745-Binding Sites,
pubmed-meshheading:17983745-Cell Line, Tumor,
pubmed-meshheading:17983745-Combinatorial Chemistry Techniques,
pubmed-meshheading:17983745-Crystallography, X-Ray,
pubmed-meshheading:17983745-Drug Design,
pubmed-meshheading:17983745-Humans,
pubmed-meshheading:17983745-Kinetics,
pubmed-meshheading:17983745-Models, Molecular,
pubmed-meshheading:17983745-Protein Kinase Inhibitors,
pubmed-meshheading:17983745-Pyrazoles,
pubmed-meshheading:17983745-Receptor, Epidermal Growth Factor,
pubmed-meshheading:17983745-Structure-Activity Relationship,
pubmed-meshheading:17983745-Substrate Specificity,
pubmed-meshheading:17983745-Vascular Endothelial Growth Factor Receptor-2
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pubmed:year |
2008
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pubmed:articleTitle |
Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening.
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pubmed:affiliation |
Department of Chemistry, Faculty of Science, Gakushuin University, Tokyo 171-8588, Japan.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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