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• W4281709754 abstract "We used mechanism-informed phenotypic screening to identify and optimize compounds that phenocopy the genetic depletion of the mitotic aurora kinase B (AURKB) kinase. After assaying nine aryl fused seven-membered lactam compounds, we identified a hit compound 6a that was subsequently optimized to five lead compounds with low nanomolar activity, represented by the lead compound 6v (19 nM). With excellent drug-like properties, these compounds reproduced the loss of function in phenotypes of AURKB and exhibited potent cytotoxic activities in various cancer cell lines. Collectively, these data support that seven-membered lactam-based analogs might be valuable for further development as a new type of antimitotic agents for the treatment of cancer." @default.
• W4281709754 created "2022-06-13" @default.
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• W4281709754 date "2022-06-06" @default.
• W4281709754 modified "2023-09-27" @default.
• W4281709754 title "Discovery and Optimization of Seven-Membered Lactam-Based Compounds to Phenocopy the Inhibition of the Aurora Kinase B" @default.
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• W4281709754 doi "https://doi.org/10.1021/acsmedchemlett.2c00098" @default.
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