dc.contributor.author | Reiersølmoen, Ann Christin | |
dc.contributor.author | Aarhus, Thomas Ihle | |
dc.contributor.author | Eckelt, Sarah | |
dc.contributor.author | Nørsett, Kristin Gabestad | |
dc.contributor.author | Sundby, Eirik | |
dc.contributor.author | Hoff, Bård Helge | |
dc.date.accessioned | 2020-01-08T09:30:13Z | |
dc.date.available | 2020-01-08T09:30:13Z | |
dc.date.created | 2019-12-11T13:22:40Z | |
dc.date.issued | 2019 | |
dc.identifier.issn | 0960-894X | |
dc.identifier.uri | http://hdl.handle.net/11250/2635253 | |
dc.description.abstract | The epidermal growth factor receptor represents an important target in cancer therapy, and low molecular weight inhibitors based on quinazolines have reached the marked. Herein we report on a new scaffold, 5-aryl-7H-pyrrolo[2,3-d]pyrimidin-4-amines, and show that when employing (S)-phenylglycinol as C-4 substituent, potent inhibitors can be made. The two most active inhibitors have suitable druglike properties, were equipotent with Erlotinib in Ba/F3 cell studies, and showed lower cross reactivity than Erlotinib in a panel of 50 kinases. | nb_NO |
dc.language.iso | eng | nb_NO |
dc.publisher | Elsevier | 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 | Potent and selective EGFR inhibitors based on 5-aryl-7H-pyrrolopyrimidin-4-amines | nb_NO |
dc.type | Journal article | nb_NO |
dc.type | Peer reviewed | nb_NO |
dc.description.version | publishedVersion | nb_NO |
dc.source.volume | 88 | nb_NO |
dc.source.journal | Bioorganic & Medicinal Chemistry Letters | nb_NO |
dc.identifier.doi | 10.1016/j.bioorg.2019.102918 | |
dc.identifier.cristin | 1759307 | |
dc.description.localcode | Copyright 2019 The Authors. Published by Elsevier Inc. This is an open access article under the CC BY-NC-ND 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.unitcode | 194,66,40,0 | |
cristin.unitname | Institutt for kjemi | |
cristin.unitname | Institutt for materialteknologi | |
cristin.unitname | Institutt for bioingeniørfag | |
cristin.ispublished | true | |
cristin.fulltext | original | |
cristin.qualitycode | 1 | |