Ergosterol analogs as inhibitors of cyclin dependent kinase 8
Petros D Siapkaras1, Eirik Johansson Solum2
1Department of Chemistry, Norwegian University of Science and Technology, Høgskoleringen 5, NO-7491 Trondheim, Norway.
Steroids
|January 23, 2022
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.
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