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Synthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors

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dc.contributor.authorKang, Seok Jong-
dc.contributor.authorLee, Jung Wuk-
dc.contributor.authorChung, Shin Hyuck-
dc.contributor.authorJang, Sun Young-
dc.contributor.authorChoi, Jaeyul-
dc.contributor.authorSuh, Kwee Hyun-
dc.contributor.authorKim, Young Hoon-
dc.contributor.authorHam, Young Jin-
dc.contributor.authorMin, Kyung Hoon-
dc.date.available2019-05-28T01:38:02Z-
dc.date.issued2019-02-
dc.identifier.issn0223-5234-
dc.identifier.issn1768-3254-
dc.identifier.urihttps://scholarworks.bwise.kr/cau/handle/2019.sw.cau/18245-
dc.description.abstractTransforming growth factor-beta activated kinase-1 (TAK1) is a potential therapeutic target for cancers and inflammatory diseases. We synthesized a series of novel imidazopyrazine derivatives, which were found to exhibit potent inhibitory effect against TAK1. Compound 22a, which possesses a good pharmacokinetic profile, showed excellent in vitro kinase activity and significant in vivo efficacy in mice xenografted with SW620, a KRAS-dependent colon cancer cell line. (C) 2018 Elsevier Masson SAS. All rights reserved.-
dc.format.extent11-
dc.language영어-
dc.language.isoENG-
dc.publisherELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER-
dc.titleSynthesis and anti-tumor activity of imidazopyrazines as TAK1 inhibitors-
dc.typeArticle-
dc.identifier.doi10.1016/j.ejmech.2018.12.025-
dc.identifier.bibliographicCitationEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, v.163, pp 660 - 670-
dc.description.isOpenAccessN-
dc.identifier.wosid000458597300049-
dc.identifier.scopusid2-s2.0-85058539198-
dc.citation.endPage670-
dc.citation.startPage660-
dc.citation.titleEUROPEAN JOURNAL OF MEDICINAL CHEMISTRY-
dc.citation.volume163-
dc.type.docTypeArticle-
dc.publisher.location프랑스-
dc.subject.keywordAuthorTAK1-
dc.subject.keywordAuthorImidazopyrazine-
dc.subject.keywordAuthorColon cancer-
dc.subject.keywordPlusACTIVATED KINASE 1-
dc.subject.keywordPlusI-KAPPA-B-
dc.subject.keywordPlusDISCOVERY-
dc.subject.keywordPlusPROTEIN-
dc.subject.keywordPlusMAPKKK-
dc.subject.keywordPlusVITRO-
dc.subject.keywordPlusIL-1-
dc.subject.keywordPlusIDENTIFICATION-
dc.subject.keywordPlusOPTIMIZATION-
dc.subject.keywordPlusMUTATIONS-
dc.relation.journalResearchAreaPharmacology & Pharmacy-
dc.relation.journalWebOfScienceCategoryChemistry, Medicinal-
dc.description.journalRegisteredClasssci-
dc.description.journalRegisteredClassscie-
dc.description.journalRegisteredClassscopus-
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