Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 신윤용 | * |
dc.contributor.author | 김대기 | * |
dc.date.accessioned | 2016-08-28T12:08:18Z | - |
dc.date.available | 2016-08-28T12:08:18Z | - |
dc.date.issued | 2010 | * |
dc.identifier.issn | 0968-0896 | * |
dc.identifier.other | OAK-6612 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/220821 | - |
dc.description.abstract | A series of 4(5)-(6-methylpyridin-2-yl)imidazoles 16-19 and -pyrazoles 22-29, 33, and 34 have been synthesized and evaluated for their ALK5 inhibitory activity in an enzyme assay and in cell-based luciferase reporter assays. The 6-quinolinyl imidazole analogs 16 and 18 inhibited ALK5 phosphorylation with IC50 values of 0.026 and 0.034 μM, respectively. In a luciferase reporter assay using HaCaT cells transiently transfected with p3TP-luc reporter construct, 18 displayed 66% inhibition at 0.05 μM, while competitor compounds 2 and 3 showed 44% inhibition. The binding mode of 18 generated by flexible docking studies with ALK5:18 complex shows that it fits well into the active site cavity of ALK5 by forming broad and tight interactions. © 2010 Elsevier Ltd. All rights reserved. | * |
dc.language | English | * |
dc.title | Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-β type 1 receptor kinase inhibitors | * |
dc.type | Article | * |
dc.relation.issue | 12 | * |
dc.relation.volume | 18 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 4459 | * |
dc.relation.lastpage | 4467 | * |
dc.relation.journaltitle | Bioorganic and Medicinal Chemistry | * |
dc.identifier.doi | 10.1016/j.bmc.2010.04.071 | * |
dc.identifier.wosid | WOS:000278480900031 | * |
dc.identifier.scopusid | 2-s2.0-77953231559 | * |
dc.author.google | Kim D.-K. | * |
dc.author.google | Lee Y.-I. | * |
dc.author.google | Lee Y.W. | * |
dc.author.google | Dewang P.M. | * |
dc.author.google | Sheen Y.Y. | * |
dc.author.google | Kim Y.W. | * |
dc.author.google | Park H.-J. | * |
dc.author.google | Yoo J. | * |
dc.author.google | Lee H.S. | * |
dc.author.google | Kim Y.-K. | * |
dc.contributor.scopusid | 신윤용(6603872711) | * |
dc.contributor.scopusid | 김대기(35083694200) | * |
dc.date.modifydate | 20240118164500 | * |