Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 신윤용 | * |
dc.contributor.author | 김대기 | * |
dc.date.accessioned | 2016-08-27T04:08:25Z | - |
dc.date.available | 2016-08-27T04:08:25Z | - |
dc.date.issued | 2015 | * |
dc.identifier.issn | 0960-894X | * |
dc.identifier.issn | 1464-3405 | * |
dc.identifier.other | OAK-15900 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/217755 | - |
dc.description.abstract | To further optimize a clinical candidate 5 (EW-7197), a series of 5-(3-, 4-, or 5-fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)imidazoles 19a-l have been synthesized and evaluated for their TGF-beta type I receptor kinase (ALK5) and p38 alpha MAP kinase inhibitory activity in an enzyme assay. The 5-(5-fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4] triazolo[1,5-a] pyridin-6-yl)imidazoles 19h-1 displayed the similar level of potency to that of 5 against both ALK5 (IC50 = 7.68-13.70 nM) and p38 alpha MAP kinase (IC50 = 1240-3370 nM). Among them, 19j inhibited ALK5 with IC50 value of 7.68 nM in a kinase assay and displayed 82% inhibition at 100 nM in a luciferase reporter assay. (C) 2015 Elsevier Ltd. All rights reserved. | * |
dc.language | English | * |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | * |
dc.subject | TGF-beta | * |
dc.subject | ALK5 inhibitor | * |
dc.subject | Fibrosis | * |
dc.subject | Cancer | * |
dc.subject | Kinase assay | * |
dc.title | Synthesis and biological evaluation of 5-(fluoro-substituted-6-methylpyridin-2-yl)-4-([1,2,4]triazolo[1,5-alpha]pyridin-6-yl)imidazoles as inhibitors of transforming growth factor-beta type I receptor kinase | * |
dc.type | Article | * |
dc.relation.issue | 22 | * |
dc.relation.volume | 25 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 5228 | * |
dc.relation.lastpage | 5231 | * |
dc.relation.journaltitle | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | * |
dc.identifier.doi | 10.1016/j.bmcl.2015.09.058 | * |
dc.identifier.wosid | WOS:000364535000043 | * |
dc.identifier.scopusid | 2-s2.0-84945963071 | * |
dc.author.google | Krishnaiah, Maddeboina | * |
dc.author.google | Jin, Cheng Hua | * |
dc.author.google | Sheen, Yhun Yhong | * |
dc.author.google | Kim, Dae-Kee | * |
dc.contributor.scopusid | 신윤용(6603872711) | * |
dc.contributor.scopusid | 김대기(35083694200) | * |
dc.date.modifydate | 20240118164500 | * |