DC Field | Value | Language |
---|---|---|
dc.contributor.author | Hong, S | ko |
dc.contributor.author | Lee, S | ko |
dc.contributor.author | Kim, B | ko |
dc.contributor.author | Lee, H | ko |
dc.contributor.author | Hong, SS | ko |
dc.contributor.author | Hong, Sungwoo | ko |
dc.date.accessioned | 2013-08-08T05:25:54Z | - |
dc.date.available | 2013-08-08T05:25:54Z | - |
dc.date.created | 2012-02-06 | - |
dc.date.created | 2012-02-06 | - |
dc.date.issued | 2010-12 | - |
dc.identifier.citation | BIOORGANIC MEDICINAL CHEMISTRY LETTERS, v.20, no.24, pp.7212 - 7215 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | http://hdl.handle.net/10203/174455 | - |
dc.description.abstract | Phosphatidylinositol-3-kinase alpha (PI3K alpha) is an important target in cancer due to the deregulation of the PI3K/AKT signaling pathway in many tumors. In this study, we designed [3,5-d]-7-azaindole analogs as PI3K alpha inhibitors through the fragment-growing strategy. By varying groups at the 3,5-positions of azaindole, we developed the SAR (Structure-activity relationship) and identified a series of potent PI3K alpha inhibitors. Representative azaindole derivatives showed activity in a cellular proliferation and apoptosis assays. Moreover, B3 exhibited strong antiangiogenic effects on cancer cells. (C) 2010 Elsevier Ltd. All rights reserved. | - |
dc.language | English | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | PHOSPHOINOSITIDE 3-KINASE | - |
dc.subject | POTENT | - |
dc.subject | ANGIOGENESIS | - |
dc.subject | KINASE | - |
dc.subject | MUTATIONS | - |
dc.subject | RAPAMYCIN | - |
dc.subject | TARGET | - |
dc.subject | PI3K | - |
dc.subject | IDENTIFICATION | - |
dc.subject | DERIVATIVES | - |
dc.title | Discovery of new azaindole-based PI3K alpha inhibitors: Apoptotic and antiangiogenic effect on cancer cells | - |
dc.type | Article | - |
dc.identifier.wosid | 000284332900004 | - |
dc.identifier.scopusid | 2-s2.0-78449274341 | - |
dc.type.rims | ART | - |
dc.citation.volume | 20 | - |
dc.citation.issue | 24 | - |
dc.citation.beginningpage | 7212 | - |
dc.citation.endingpage | 7215 | - |
dc.citation.publicationname | BIOORGANIC MEDICINAL CHEMISTRY LETTERS | - |
dc.identifier.doi | 10.1016/j.bmcl.2010.10.108 | - |
dc.contributor.localauthor | Hong, Sungwoo | - |
dc.contributor.nonIdAuthor | Lee, H | - |
dc.contributor.nonIdAuthor | Hong, SS | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | Phosphatidylinositol-3-kinase | - |
dc.subject.keywordAuthor | Azaindole | - |
dc.subject.keywordAuthor | Fragment-growing strategy | - |
dc.subject.keywordAuthor | Antiangiogenesis | - |
dc.subject.keywordPlus | PHOSPHOINOSITIDE 3-KINASE | - |
dc.subject.keywordPlus | POTENT | - |
dc.subject.keywordPlus | ANGIOGENESIS | - |
dc.subject.keywordPlus | KINASE | - |
dc.subject.keywordPlus | MUTATIONS | - |
dc.subject.keywordPlus | RAPAMYCIN | - |
dc.subject.keywordPlus | TARGET | - |
dc.subject.keywordPlus | PI3K | - |
dc.subject.keywordPlus | IDENTIFICATION | - |
dc.subject.keywordPlus | DERIVATIVES | - |
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