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- W3113935145 abstract "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." @default.
- W3113935145 created "2021-01-05" @default.
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- W3113935145 date "2020-12-16" @default.
- W3113935145 modified "2023-10-18" @default.
- W3113935145 title "Cyclopenta[<i>b</i>]indole Derivative Inhibits Aurora B in Primary Cells" @default.
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- W3113935145 doi "https://doi.org/10.1021/acsomega.0c05491" @default.
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