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- W2000767526 abstract "The o-carboxylic acid substituted bisanilinopyrimidine 1 was identified as a potent hit (Aurora A IC50 = 6.1 ± 1.0 nM) from in-house screening. Detailed structure–activity relationship (SAR) studies indicated that polar substituents at the para position of the B-ring are critical for potent activity. X-ray crystallography studies revealed that compound 1 is a type I inhibitor that binds the Aurora kinase active site in a DFG-in conformation. Structure–activity guided replacement of the A-ring carboxylic acid with halogens and incorporation of fluorine at the pyrimidine 5-position led to highly potent inhibitors of Aurora A that bind in a DFG-out conformation. B-Ring modifications were undertaken to improve the solubility and cell permeability. Compounds such as 9m with water-solubilizing moieties at the para position of the B-ring inhibited the autophosphorylation of Aurora A in MDA-MB-468 breast cancer cells." @default.
- W2000767526 created "2016-06-24" @default.
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- W2000767526 date "2012-08-30" @default.
- W2000767526 modified "2023-10-18" @default.
- W2000767526 title "Development of <i>o</i>-Chlorophenyl Substituted Pyrimidines as Exceptionally Potent Aurora Kinase Inhibitors" @default.
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- W2000767526 doi "https://doi.org/10.1021/jm300334d" @default.
- W2000767526 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4429609" @default.
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- W2000767526 hasPublicationYear "2012" @default.
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