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dc.contributor.authorSolum, Eirik Johansson
dc.contributor.authorHansen, Trond Vidar
dc.contributor.authorAesoy, Reidun
dc.contributor.authorHerfindal, Lars
dc.date.accessioned2020-07-09T11:58:19Z
dc.date.available2020-07-09T11:58:19Z
dc.date.created2020-04-30T09:07:52Z
dc.date.issued2020
dc.identifier.citationSolum, E. J., Hansen, T. V., Aesoy, R. & Herfindal, L. (2020). New CDK8 inhibitors as potential anti-leukemic agents – Design, synthesisand biological evaluation. Bioorganic & Medicinal Chemistry, 28(10): 115461. doi:en_US
dc.identifier.issn1464-3391
dc.identifier.urihttps://hdl.handle.net/11250/2661805
dc.description.abstractCyclin-dependent kinase 8 (CDK8) plays a vital role in regulating cell transcription either through its association with the mediator complex or by the phosphorylation of transcription factors. CDK8-mediated activation of oncogenes has proved to be important in a variety of cancer types including hematological malignancies. We have designed and synthesized a series of new synthetic steroids. The compounds were evaluated as CDK8 inhibitors in vitro. The three most potent compounds exhibit Kd-values towards CDK8 in the low nanomolar range (3.5–18 nM). Furthermore, the compounds displayed selectivity for CDK8 in a panel of 465 different kinases. The cell studies indicated a selectivity to kill AML-cancer cell lines compared to normal cell lines.en_US
dc.language.isoengen_US
dc.publisherElsevieren_US
dc.rightsNavngivelse 4.0 Internasjonal*
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/deed.no*
dc.titleNew CDK8 inhibitors as potential anti-leukemic agents – Design, synthesisand biological evaluationen_US
dc.typePeer revieweden_US
dc.typeJournal articleen_US
dc.description.versionpublishedVersionen_US
dc.rights.holder© 2020 The Author(s)en_US
dc.subject.nsiVDP::Medisinske Fag: 700::Basale medisinske, odontologiske og veterinærmedisinske fag: 710::Medisinsk molekylærbiologi: 711en_US
dc.source.pagenumber8en_US
dc.source.volume28en_US
dc.source.journalBioorganic & Medicinal Chemistryen_US
dc.source.issue10en_US
dc.identifier.doi10.1016/j.bmc.2020.115461
dc.identifier.cristin1808756
dc.description.localcodeUnit Licence Agreementen_US


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