dc.contributor.author | Solum, Eirik Johansson | |
dc.contributor.author | Hansen, Trond Vidar | |
dc.contributor.author | Æsøy, Reidun | |
dc.contributor.author | Herfindal, Lars | |
dc.date.accessioned | 2021-04-12T13:03:30Z | |
dc.date.available | 2021-04-12T13:03:30Z | |
dc.date.created | 2020-04-30T09:07:52Z | |
dc.date.issued | 2020 | |
dc.Published | Bioorganic & Medicinal Chemistry. 2020, 28:115461 (10), 1-8. | |
dc.identifier.issn | 0968-0896 | |
dc.identifier.uri | https://hdl.handle.net/11250/2737342 | |
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, synthesis and biological evaluation | en_US |
dc.type | Journal article | en_US |
dc.type | Peer reviewed | en_US |
dc.description.version | publishedVersion | en_US |
dc.rights.holder | Copyright 2020 The Authors. | en_US |
dc.source.articlenumber | 115461 | en_US |
cristin.ispublished | true | |
cristin.fulltext | original | |
cristin.qualitycode | 1 | |
dc.identifier.doi | 10.1016/j.bmc.2020.115461 | |
dc.identifier.cristin | 1808756 | |
dc.source.journal | Bioorganic & Medicinal Chemistry | en_US |
dc.source.40 | 28:115461 | |
dc.source.14 | 10 | |
dc.identifier.citation | Bioorganic & Medicinal Chemistry. 2020, 28 (10), 115461. | en_US |
dc.source.volume | 28 | en_US |
dc.source.issue | 10 | en_US |