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dc.contributor.authorChoi, Hwan Geun-
dc.contributor.authorZhang, Jianming-
dc.contributor.authorWeisberg, Ellen-
dc.contributor.authorGriffin, James D.-
dc.contributor.authorSim, Taebo-
dc.contributor.authorGray, Nathanael S.-
dc.date.accessioned2024-01-20T14:04:11Z-
dc.date.available2024-01-20T14:04:11Z-
dc.date.created2021-09-05-
dc.date.issued2012-08-15-
dc.identifier.issn0960-894X-
dc.identifier.urihttps://pubs.kist.re.kr/handle/201004/128973-
dc.description.abstractHG-7-85-01(22) and HG-7-86-01(26) are thiazolo[5,4-b]pyridine containing type II tyrosine kinase inhibitors with potent cellular activity against both wild-type and 'gatekeeper' mutant T315I-Bcr-Abl. Here we report on the 'hybrid design' concept and subsequent structure activity guided optimization efforts that resulted in the development of these inhibitors. (C) 2012 Elsevier Ltd. All rights reserved.-
dc.languageEnglish-
dc.publisherPergamon Press Ltd.-
dc.subjectCHRONIC MYELOID-LEUKEMIA-
dc.subjectABL TYROSINE KINASE-
dc.subjectBCR-ABL-
dc.subjectSELECTIVE INHIBITOR-
dc.subjectRESISTANCE-
dc.subjectDISCOVERY-
dc.subjectIMATINIB-
dc.subjectSRC-
dc.subjectAMN107-
dc.subjectCELLS-
dc.titleDevelopment of 'DFG-out' inhibitors of gatekeeper mutant kinases-
dc.typeArticle-
dc.identifier.doi10.1016/j.bmcl.2012.06.036-
dc.description.journalClass1-
dc.identifier.bibliographicCitationBioorganic & Medicinal Chemistry Letters, v.22, no.16, pp.5297 - 5302-
dc.citation.titleBioorganic & Medicinal Chemistry Letters-
dc.citation.volume22-
dc.citation.number16-
dc.citation.startPage5297-
dc.citation.endPage5302-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
dc.identifier.wosid000306962800028-
dc.identifier.scopusid2-s2.0-84864403909-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.relation.journalWebOfScienceCategoryChemistry, Organic-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalResearchAreaChemistry-
dc.type.docTypeArticle-
dc.subject.keywordPlusCHRONIC MYELOID-LEUKEMIA-
dc.subject.keywordPlusABL TYROSINE KINASE-
dc.subject.keywordPlusBCR-ABL-
dc.subject.keywordPlusSELECTIVE INHIBITOR-
dc.subject.keywordPlusRESISTANCE-
dc.subject.keywordPlusDISCOVERY-
dc.subject.keywordPlusIMATINIB-
dc.subject.keywordPlusSRC-
dc.subject.keywordPlusAMN107-
dc.subject.keywordPlusCELLS-
dc.subject.keywordAuthorT315I Bcr-Abl-
dc.subject.keywordAuthorKinase inhibitor-
dc.subject.keywordAuthorGatekeeper mutant-
dc.subject.keywordAuthorType II inhibitor-
dc.subject.keywordAuthorThiazolo[5,4-b]pyridine-
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