| Literature DB >> 35065996 |
Petros D Siapkaras1, Eirik Johansson Solum2.
Abstract
Five new compounds based on the structure of ergosterol have been prepared and tested for their ability to inhibit CDK8. The design of the compounds was inspired by the previous reported CDK8 inhibitors, cortistatin A, CCT251921 and Senexin A. The two most potent compounds, 16a and 16d, inhibited the target enzyme with Kd-values of 107 and 93 nM, respectively.Entities:
Keywords: CDK8-inhibition; Cortistatin A; Ergosterol; Heck-reaction; Steroids
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Year: 2022 PMID： 35065996 DOI： 10.1016/j.steroids.2022.108965
Source DB: PubMed Journal: Steroids ISSN： 0039-128X Impact factor: 2.668