Cyclopenta[ b]indole Derivative Inhibits Aurora B in Primary Cells
Artikel i vetenskaplig tidskrift, 2020

The Aurora family of kinases is closely involved in regulating cell division. Inhibition of Aurora A and B with small molecules is currently being investigated in clinical trials for the treatment of different cancers. It has also been evaluated as a treatment option against different autoimmune diseases in preclinical studies. Here, we present a cyclopenta[b]indole derivative capable of inhibiting Aurora B selectively in kinase assays. To evaluate the Aurora B inhibition capacity of the compound, we used a kinase IC50 assay as well as a suppression assay of proliferating primary cells. In addition, we examined if the cells had gained a phenotype characteristic for Aurora B inhibition after treatment with the compound. We found that the compound selectively inhibited Aurora B (IC50 = 1.4 μM) over Aurora A (IC50 > 30 μM). Moreover, the compound inhibited proliferating PBMCs with an IC50 = 4.2 μM, and the cells displayed reduced phosphorylation of histone H3 as well as tetraploidy, consistent with Aurora B inhibition.


Andreas Ekebergh

Chalmers, Kemi och kemiteknik, Kemi och biokemi

Jerker Mårtensson

Chalmers, Kemi och kemiteknik, Kemi och biokemi

Christine Lingblom Ekebergh

Göteborgs universitet

Sahlgrenska universitetssjukhuset

ACS Omega

24701343 (eISSN)

Vol. 5 51 33455-33460


Cell- och molekylärbiologi

Farmakologi och toxikologi

Medicinsk bioteknologi (med inriktning mot cellbiologi (inklusive stamcellsbiologi), molekylärbiologi, mikrobiologi, biokemi eller biofarmaci)





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