Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-beta type 1 receptor ldnase inhibitors
DC Field | Value | Language |
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dc.contributor.author | Li, Fei | - |
dc.contributor.author | Park, Yunjeong | - |
dc.contributor.author | Hah, Jung-Mi | - |
dc.contributor.author | Ryu, Jae-Sang | - |
dc.date.accessioned | 2021-06-23T04:03:49Z | - |
dc.date.available | 2021-06-23T04:03:49Z | - |
dc.date.created | 2021-01-21 | - |
dc.date.issued | 2013-02 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/28854 | - |
dc.description.abstract | A series of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles has been synthesized and evaluated for their ALK5 inhibitory activity. The 1-(6-methylpyridin-2-yl)-1,2,3-triazoles were assembled by Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition. Following this, quinoxaline was introduced through Pd-catalyzed direct arylation. The synthesized 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles revealed significant selectivity differences with respect to p38 alpha MAP kinase. In particular, 12k showed 80.8% ALK5 inhibitory activity at a concentration of 10 mu M and IC50 value of 4.69 mu M, but did not show p38 alpha MAP kinase inhibitory activity (-1.94% inhibition at a concentration of 10 mu M). (C) 2012 Elsevier Ltd. All rights reserved. | - |
dc.language | 영어 | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.title | Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor-beta type 1 receptor ldnase inhibitors | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Hah, Jung-Mi | - |
dc.identifier.doi | 10.1016/j.bmcl.2012.12.008 | - |
dc.identifier.scopusid | 2-s2.0-84872939277 | - |
dc.identifier.wosid | 000314625400032 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.23, no.4, pp.1083 - 1086 | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 23 | - |
dc.citation.number | 4 | - |
dc.citation.startPage | 1083 | - |
dc.citation.endPage | 1086 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.isOpenAccess | N | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.subject.keywordPlus | TGF-BETA | - |
dc.subject.keywordPlus | SIGNAL-TRANSDUCTION | - |
dc.subject.keywordPlus | ALK5 INHIBITOR | - |
dc.subject.keywordPlus | KINASE-5 | - |
dc.subject.keywordPlus | FIBROSIS | - |
dc.subject.keywordPlus | IN-1130 | - |
dc.subject.keywordPlus | DISEASE | - |
dc.subject.keywordPlus | 1,2,3-TRIAZOLES | - |
dc.subject.keywordPlus | PREVENTION | - |
dc.subject.keywordPlus | CANCER | - |
dc.subject.keywordAuthor | ALK5 | - |
dc.subject.keywordAuthor | TGF-beta type 1 receptor kinase | - |
dc.subject.keywordAuthor | Anticancer | - |
dc.subject.keywordAuthor | Click chemistry | - |
dc.subject.keywordAuthor | 1,2,3-Triazole | - |
dc.identifier.url | https://www.sciencedirect.com/science/article/pii/S0960894X12015922?via%3Dihub | - |
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