Design, Synthesis, and Evaluation of 3,5-Disubstituted 7-Azaindoles as Trk Inhibitors with Anticancer and Antiangiogenic Activities

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dc.contributor.authorHong, Seungheeko
dc.contributor.authorKim, Jinheeko
dc.contributor.authorSeo, Ju Hyeonko
dc.contributor.authorJung, Kyung Heeko
dc.contributor.authorHong, Soon-Sunko
dc.contributor.authorHong, Sungwooko
dc.date.accessioned2013-03-12T12:36:35Z-
dc.date.available2013-03-12T12:36:35Z-
dc.date.created2012-08-14-
dc.date.created2012-08-14-
dc.date.issued2012-06-
dc.identifier.citationJOURNAL OF MEDICINAL CHEMISTRY, v.55, no.11, pp.5337 - 5349-
dc.identifier.issn0022-2623-
dc.identifier.urihttp://hdl.handle.net/10203/102345-
dc.description.abstractTropomyosin-related kinase A (TrkA) is considered a promising target in the development of a therapeutic treatment of cancer and pain. In this study, we designed and synthesized a series of novel 7-azaindole-based Trk kinase inhibitors through the structure-based design strategy. By varying the functional groups at the 3 and 5 positions of a 7-azaindole scaffold, we studied the structure-activity relationships (SAR) profiles and identified a series of potent Trk inhibitors. Representative derivatives showed desirable activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited noteworthy antiangiogenic activity.-
dc.languageEnglish-
dc.publisherAMER CHEMICAL SOC-
dc.subjectNERVE GROWTH-FACTOR-
dc.subjectKINASE INHIBITORS-
dc.subjectBREAST-CANCER-
dc.subjectIDENTIFICATION-
dc.subjectMETASTASIS-
dc.subjectDISCOVERY-
dc.subjectCELLS-
dc.titleDesign, Synthesis, and Evaluation of 3,5-Disubstituted 7-Azaindoles as Trk Inhibitors with Anticancer and Antiangiogenic Activities-
dc.typeArticle-
dc.identifier.wosid000305356400033-
dc.identifier.scopusid2-s2.0-84862280700-
dc.type.rimsART-
dc.citation.volume55-
dc.citation.issue11-
dc.citation.beginningpage5337-
dc.citation.endingpage5349-
dc.citation.publicationnameJOURNAL OF MEDICINAL CHEMISTRY-
dc.identifier.doi10.1021/jm3002982-
dc.contributor.localauthorHong, Sungwoo-
dc.contributor.nonIdAuthorSeo, Ju Hyeon-
dc.contributor.nonIdAuthorJung, Kyung Hee-
dc.contributor.nonIdAuthorHong, Soon-Sun-
dc.type.journalArticleArticle-
dc.subject.keywordPlusNERVE GROWTH-FACTOR-
dc.subject.keywordPlusKINASE INHIBITORS-
dc.subject.keywordPlusBREAST-CANCER-
dc.subject.keywordPlusIDENTIFICATION-
dc.subject.keywordPlusMETASTASIS-
dc.subject.keywordPlusDISCOVERY-
dc.subject.keywordPlusCELLS-
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