Source:http://linkedlifedata.com/resource/pubmed/id/21316229
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| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
6
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| pubmed:dateCreated |
2011-3-7
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| pubmed:abstractText |
Phosphatidylinositol 3-kinase (PI3K) is a lipid kinase and a promising therapeutic target for cancer. Using structure-based drug design (SBDD), we have identified novel PI3K inhibitors with a dihydropyrrolopyrimidine skeleton. Metabolic stability of the first lead series was drastically improved by replacing phenol with aminopyrimidine moiety. CH5132799, a novel class I PI3K inhibitor, exhibited a strong inhibitory activity especially against PI3K? (IC(50)=0.014 ?M). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice.
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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
|
| pubmed:month |
Mar
|
| pubmed:issn |
1464-3405
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| pubmed:author |
pubmed-author:AokiYukoY,
pubmed-author:EbiikeHirosatoH,
pubmed-author:KawadaHatsuoH,
pubmed-author:KondohOsamuO,
pubmed-author:KuramotoShinoS,
pubmed-author:MiyazakiTakuyaT,
pubmed-author:MorikamiKenjiK,
pubmed-author:NakamuraMitsuakiM,
pubmed-author:OgawaKotaroK,
pubmed-author:OhwadaJunJ,
pubmed-author:ShimmaNobuoN,
pubmed-author:TsukazakiMasaoM,
pubmed-author:YoshidaMiyukiM,
pubmed-author:YoshinariKiyoshiK
|
| pubmed:copyrightInfo |
Copyright © 2011 Elsevier Ltd. All rights reserved.
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| pubmed:issnType |
Electronic
|
| pubmed:day |
15
|
| pubmed:volume |
21
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
1767-72
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| pubmed:meshHeading |
pubmed-meshheading:21316229-Cell Line, Tumor,
pubmed-meshheading:21316229-Enzyme Inhibitors,
pubmed-meshheading:21316229-Humans,
pubmed-meshheading:21316229-Models, Molecular,
pubmed-meshheading:21316229-Phosphatidylinositol 3-Kinases,
pubmed-meshheading:21316229-Pyrimidines,
pubmed-meshheading:21316229-Sulfonamides
|
| pubmed:year |
2011
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| pubmed:articleTitle |
Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799.
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| pubmed:affiliation |
Research Division, Chugai Pharmaceutical Co., Ltd , Kamakura, Kanagawa, Japan. ohwadajn@chugai-pharm.co.jp
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| pubmed:publicationType |
Journal Article
|