Design and Synthesis of Imidazopyridine Analogues as Inhibitors of Phosphoinositide 3-Kinase Signaling and Angiogenesis

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dc.contributor.authorKim, Oko
dc.contributor.authorJeong, Yko
dc.contributor.authorLee, Hko
dc.contributor.authorHong, SSko
dc.contributor.authorHong, Sungwooko
dc.date.accessioned2013-03-11T01:11:47Z-
dc.date.available2013-03-11T01:11:47Z-
dc.date.created2012-02-06-
dc.date.created2012-02-06-
dc.date.issued2011-04-
dc.identifier.citationJOURNAL OF MEDICINAL CHEMISTRY, v.54, no.7, pp.2455 - 2466-
dc.identifier.issn0022-2623-
dc.identifier.urihttp://hdl.handle.net/10203/97883-
dc.description.abstractPhosphatidylinositol 3-kinase alpha (P13K alpha) is an important regulator of intracellular signaling pathways, controlling remarkably diverse arrays of physiological processes. Because the P13K pathway is frequently up-regulated in human cancers, the inhibition of P13K alpha can be a promising approach to cancer therapy. In this study, we have designed and synthesized a new series of imidazo[1,2-a]pyridine derivatives as P13K alpha inhibitors through the fragment-growing strategy. By varying groups at the 3- and 6-positions of imidazo[1,2-a]pyridines, we studied the structure-activity relationships (SAR) profiles and identified a series of potent P13K alpha inhibitors. Representative derivatives showed good activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited note-worthy antiangiogenic activity.-
dc.languageEnglish-
dc.publisherAMER CHEMICAL SOC-
dc.subjectENDOTHELIAL GROWTH-FACTOR-
dc.subjectIN-VIVO-
dc.subjectCANCER-
dc.subjectPOTENT-
dc.subjectIDENTIFICATION-
dc.subjectMUTATIONS-
dc.subjectDISCOVERY-
dc.subjectRAPAMYCIN-
dc.subjectISOFORM-
dc.subjectPATHWAY-
dc.titleDesign and Synthesis of Imidazopyridine Analogues as Inhibitors of Phosphoinositide 3-Kinase Signaling and Angiogenesis-
dc.typeArticle-
dc.identifier.wosid000289215700041-
dc.identifier.scopusid2-s2.0-79953777821-
dc.type.rimsART-
dc.citation.volume54-
dc.citation.issue7-
dc.citation.beginningpage2455-
dc.citation.endingpage2466-
dc.citation.publicationnameJOURNAL OF MEDICINAL CHEMISTRY-
dc.identifier.doi10.1021/jm101582z-
dc.contributor.localauthorHong, Sungwoo-
dc.contributor.nonIdAuthorLee, H-
dc.contributor.nonIdAuthorHong, SS-
dc.type.journalArticleArticle-
dc.subject.keywordPlusENDOTHELIAL GROWTH-FACTOR-
dc.subject.keywordPlusIN-VIVO-
dc.subject.keywordPlusCANCER-
dc.subject.keywordPlusPOTENT-
dc.subject.keywordPlusIDENTIFICATION-
dc.subject.keywordPlusMUTATIONS-
dc.subject.keywordPlusDISCOVERY-
dc.subject.keywordPlusRAPAMYCIN-
dc.subject.keywordPlusISOFORM-
dc.subject.keywordPlusPATHWAY-
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