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• W4302425185 endingPage "1804" @default.
• W4302425185 startingPage "1797" @default.
• W4302425185 abstract "A series of exceptionally selective CDK2 inhibitors are described. Starting from an HTS hit, we successfully scaffold hopped to a 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one core structure, which imparted a promising initial selectivity within the CDK family. Extensive further SAR identified additional factors that drove selectivity to above 200× for CDKs 1/4/6/7/9. General kinome selectivity was also greatly improved. Finally, use of in vivo metabolite identification allowed us to pinpoint sulfonamide dealkylation as the primary metabolite, which was ameliorated through the deuterium effect." @default.
• W4302425185 created "2022-10-06" @default.
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• W4302425185 date "2022-10-06" @default.
• W4302425185 modified "2023-09-27" @default.
• W4302425185 title "Discovery of 5,7-Dihydro-6<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-6-ones as Highly Selective CDK2 Inhibitors" @default.
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• W4302425185 doi "https://doi.org/10.1021/acsmedchemlett.2c00408" @default.
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