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dc.contributor.authorReiersølmoen, Ann Christin
dc.contributor.authorAarhus, Thomas Ihle
dc.contributor.authorEckelt, Sarah
dc.contributor.authorNørsett, Kristin Gabestad
dc.contributor.authorSundby, Eirik
dc.contributor.authorHoff, Bård Helge
dc.date.accessioned2020-01-08T09:30:13Z
dc.date.available2020-01-08T09:30:13Z
dc.date.created2019-12-11T13:22:40Z
dc.date.issued2019
dc.identifier.issn0960-894X
dc.identifier.urihttp://hdl.handle.net/11250/2635253
dc.description.abstractThe 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.isoengnb_NO
dc.publisherElseviernb_NO
dc.rightsAttribution-NonCommercial-NoDerivatives 4.0 Internasjonal*
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/deed.no*
dc.titlePotent and selective EGFR inhibitors based on 5-aryl-7H-pyrrolopyrimidin-4-aminesnb_NO
dc.typeJournal articlenb_NO
dc.typePeer reviewednb_NO
dc.description.versionpublishedVersionnb_NO
dc.source.volume88nb_NO
dc.source.journalBioorganic & Medicinal Chemistry Lettersnb_NO
dc.identifier.doi10.1016/j.bioorg.2019.102918
dc.identifier.cristin1759307
dc.description.localcodeCopyright 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.unitcode194,66,25,0
cristin.unitcode194,66,35,0
cristin.unitcode194,66,40,0
cristin.unitnameInstitutt for kjemi
cristin.unitnameInstitutt for materialteknologi
cristin.unitnameInstitutt for bioingeniørfag
cristin.ispublishedtrue
cristin.fulltextoriginal
cristin.qualitycode1


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Attribution-NonCommercial-NoDerivatives 4.0 Internasjonal
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