Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 하정미 | - |
dc.date.accessioned | 2023-08-23T01:14:15Z | - |
dc.date.available | 2023-08-23T01:14:15Z | - |
dc.date.issued | 2013-02 | - |
dc.identifier.citation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v. 23, NO. 4, Page. 1083-1086 | - |
dc.identifier.issn | 0960-894X;1464-3405 | - |
dc.identifier.uri | https://www.sciencedirect.com/science/article/pii/S0960894X12015922?via%3Dihub | en_US |
dc.identifier.uri | https://repository.hanyang.ac.kr/handle/20.500.11754/186130 | - |
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 | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | ALK5 | - |
dc.subject | TGF-beta type 1 receptor kinase | - |
dc.subject | Anticancer | - |
dc.subject | Click chemistry | - |
dc.subject | 1,2,3-Triazole | - |
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.relation.no | 4 | - |
dc.relation.volume | 23 | - |
dc.identifier.doi | 10.1016/j.bmcl.2012.12.008 | - |
dc.relation.page | 1083-1086 | - |
dc.relation.journal | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.contributor.googleauthor | Li, Fei | - |
dc.contributor.googleauthor | Park, Yunjeong | - |
dc.contributor.googleauthor | Hah, Jung-Mi | - |
dc.contributor.googleauthor | Ryu, Jae-Sang | - |
dc.sector.campus | E | - |
dc.sector.daehak | 약학대학 | - |
dc.sector.department | 약학과 | - |
dc.identifier.pid | jhah | - |
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