Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 이화정 | * |
dc.contributor.author | 김대기 | * |
dc.date.accessioned | 2020-04-06T16:30:07Z | - |
dc.date.available | 2020-04-06T16:30:07Z | - |
dc.date.issued | 2020 | * |
dc.identifier.issn | 1475-6366 | * |
dc.identifier.issn | 1475-6374 | * |
dc.identifier.other | OAK-26676 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/253722 | - |
dc.description.abstract | A series of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles, 7a-c, 11a-h, and 16a-h has been synthesised and evaluated for their ALK5 inhibitory activity in an enzyme assay and in a cell-based luciferase reporter assay. Incorporation of a quinoxalin-6-yl moiety and a methylene linker at the 4- and 2-position of the imidazole ring, respectively, and a m-CONH2 substituent in the phenyl ring generated a highly potent and selective ALK5 inhibitor 11e. Docking model of ALK5 in complex with 11e showed that it fitted well in the ATP-binding pocket with favourable interactions. | * |
dc.language | English | * |
dc.publisher | TAYLOR & | * |
dc.publisher | FRANCIS LTD | * |
dc.subject | 2 | * |
dc.subject | 4-Disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles | * |
dc.subject | ALK5 inhibition | * |
dc.subject | cancer immunotherapeutic agent | * |
dc.subject | docking | * |
dc.title | Synthesis, biological evaluation and molecular modelling of 2,4-disubstituted-5-(6-alkylpyridin-2-yl)-1H-imidazoles as ALK5 inhibitors | * |
dc.type | Article | * |
dc.relation.issue | 1 | * |
dc.relation.volume | 35 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 702 | * |
dc.relation.lastpage | 712 | * |
dc.relation.journaltitle | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | * |
dc.identifier.doi | 10.1080/14756366.2020.1734799 | * |
dc.identifier.wosid | WOS:000519283000001 | * |
dc.author.google | Park, Myoung-Soon | * |
dc.author.google | Park, Hyun-Ju | * |
dc.author.google | An, Young Jae | * |
dc.author.google | Choi, Joon Hun | * |
dc.author.google | Cha, Geunyoung | * |
dc.author.google | Lee, Hwa Jeong | * |
dc.author.google | Park, So-Jung | * |
dc.author.google | Dewang, Purushottam M. | * |
dc.author.google | Kim, Dae-Kee | * |
dc.contributor.scopusid | 이화정(57102029300) | * |
dc.contributor.scopusid | 김대기(35083694200) | * |
dc.date.modifydate | 20240118154655 | * |