dc.contributor.author | Solum, Eirik Johansson | |
dc.contributor.author | Hansen, Trond Vidar | |
dc.contributor.author | Aesoy, Reidun | |
dc.contributor.author | Herfindal, Lars | |
dc.date.accessioned | 2020-07-09T11:58:19Z | |
dc.date.available | 2020-07-09T11:58:19Z | |
dc.date.created | 2020-04-30T09:07:52Z | |
dc.date.issued | 2020 | |
dc.identifier.citation | Solum, 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.issn | 1464-3391 | |
dc.identifier.uri | https://hdl.handle.net/11250/2661805 | |
dc.description.abstract | Cyclin-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.iso | eng | en_US |
dc.publisher | Elsevier | en_US |
dc.rights | Navngivelse 4.0 Internasjonal | * |
dc.rights.uri | http://creativecommons.org/licenses/by/4.0/deed.no | * |
dc.title | New CDK8 inhibitors as potential anti-leukemic agents – Design, synthesisand biological evaluation | en_US |
dc.type | Peer reviewed | en_US |
dc.type | Journal article | en_US |
dc.description.version | publishedVersion | en_US |
dc.rights.holder | © 2020 The Author(s) | en_US |
dc.subject.nsi | VDP::Medisinske Fag: 700::Basale medisinske, odontologiske og veterinærmedisinske fag: 710::Medisinsk molekylærbiologi: 711 | en_US |
dc.source.pagenumber | 8 | en_US |
dc.source.volume | 28 | en_US |
dc.source.journal | Bioorganic & Medicinal Chemistry | en_US |
dc.source.issue | 10 | en_US |
dc.identifier.doi | 10.1016/j.bmc.2020.115461 | |
dc.identifier.cristin | 1808756 | |
dc.description.localcode | Unit Licence Agreement | en_US |