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5,6-Diarylpyrazolo[1,5-a]pyrimidines are p21-dependent cyclin-dependent kinase (CDK) 2 inhibitors. This series of compounds features an N,N-dimethyl-3-methoxypropenamide moiety as a 2-position substituent. Whereas a methyl group in the N,N-dimethyl-3-methoxypropenamide moiety is a necessary feature for p21-dependent CDK2 inhibition, the larger 3-methoxypropenamide moiety could be tuned for optimal activity by the small 3-methoxypropenamide substituent, including 3-methoxymethyl, 3-methoxyethyl, 3-methoxypropyl, and 3-methoxyprop-2-enyl (3-methoxyprop-2-en-1