dc.contributor.author | Reiersølmoen, Ann Christin | |
dc.contributor.author | Han, Jin | |
dc.contributor.author | Sundby, Eirik | |
dc.contributor.author | Hoff, Bård Helge | |
dc.date.accessioned | 2019-05-28T12:49:14Z | |
dc.date.available | 2019-05-28T12:49:14Z | |
dc.date.created | 2018-11-05T20:26:54Z | |
dc.date.issued | 2018 | |
dc.identifier.citation | European Journal of Medicinal Chemistry. 2018, 155 562-578. | nb_NO |
dc.identifier.issn | 0223-5234 | |
dc.identifier.uri | http://hdl.handle.net/11250/2599282 | |
dc.description.abstract | Inhibiting the interleukin 17 pathway is of interest in a number of autoimmune diseases. Herein, 42 fused
pyrimidines have been evaluated as interleukin 17 secretion inhibitors using a phenotypic assay with
peripheral blood mononuclear cells. 7H-Pyrrolo [2,3-d]pyrimidin-4-amines having aryl groups at C-5 or
C-6 were found more active than the corresponding thieno- and furopyrimidines. Low cytotoxicity was
seen for the most active inhibitors. However, the pyrrolopyrimidines also inhibit interleukin 5 secretion,
suggesting that selective interleukin 17 inhibitors should rather be based on furopyrimidines. Profiling
towards a panel of 51 kinases and assays towards the retinoic acid receptor-related orphan receptor
gamma were performed in order to identify the compounds mode of action. | nb_NO |
dc.language.iso | eng | nb_NO |
dc.rights | Attribution-NonCommercial-NoDerivatives 4.0 Internasjonal | * |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/deed.no | * |
dc.title | Identification of fused pyrimidines as interleukin 17 secretion inhibitors | nb_NO |
dc.type | Journal article | nb_NO |
dc.type | Peer reviewed | nb_NO |
dc.description.version | acceptedVersion | nb_NO |
dc.source.pagenumber | 562-578 | nb_NO |
dc.source.volume | 155 | nb_NO |
dc.source.journal | European Journal of Medicinal Chemistry | nb_NO |
dc.identifier.doi | 10.1016/j.ejmech.2018.06.019 | |
dc.identifier.cristin | 1627244 | |
dc.description.localcode | © 2018. This is the authors’ accepted and refereed manuscript to the article. Locked until 15.06.2020 due to copyright restrictions. This manuscript version is made available under the CC-BY-NC-ND 4.0 license http://creativecommons.org/licenses/by-nc-nd/4.0/ | nb_NO |
cristin.unitcode | 194,66,25,0 | |
cristin.unitcode | 194,66,35,0 | |
cristin.unitname | Institutt for kjemi | |
cristin.unitname | Institutt for materialteknologi | |
cristin.ispublished | true | |
cristin.fulltext | preprint | |
cristin.qualitycode | 1 | |