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dc.date.accessioned2020-08-18T19:25:43Z
dc.date.available2020-08-18T19:25:43Z
dc.date.created2020-04-30T09:07:52Z
dc.date.issued2020
dc.identifier.citationSolum, Eirik Johansson Hansen, Trond Vidar Aesoy, Reidun Herfindal, Lars . New CDK8 inhibitors as potential anti-leukemic agents – Design, synthesisand biological evaluation. Bioorganic & Medicinal Chemistry. 2020, 28:115461(10), 1-8
dc.identifier.urihttp://hdl.handle.net/10852/78529
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.
dc.languageEN
dc.rightsAttribution 4.0 International
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.titleNew CDK8 inhibitors as potential anti-leukemic agents – Design, synthesisand biological evaluation
dc.typeJournal article
dc.creator.authorSolum, Eirik Johansson
dc.creator.authorHansen, Trond Vidar
dc.creator.authorAesoy, Reidun
dc.creator.authorHerfindal, Lars
cristin.unitcode185,15,23,20
cristin.unitnameSeksjon for farmasøytisk kjemi
cristin.ispublishedtrue
cristin.fulltextoriginal
cristin.qualitycode1
dc.identifier.cristin1808756
dc.identifier.bibliographiccitationinfo:ofi/fmt:kev:mtx:ctx&ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Bioorganic & Medicinal Chemistry&rft.volume=28:115461&rft.spage=1&rft.date=2020
dc.identifier.jtitleBioorganic & Medicinal Chemistry
dc.identifier.volume28
dc.identifier.issue10
dc.identifier.doihttps://doi.org/10.1016/j.bmc.2020.115461
dc.identifier.urnURN:NBN:no-81621
dc.type.documentTidsskriftartikkel
dc.type.peerreviewedPeer reviewed
dc.source.issn0968-0896
dc.identifier.fulltextFulltext https://www.duo.uio.no/bitstream/handle/10852/78529/2/Solum.pdf
dc.type.versionPublishedVersion
cristin.articleid115461


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