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New pyrazolo[1,5-a]pyrimidine derivatives as potential CDK2 inhibitors and apoptosis-driven antiproliferative agents
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DOI：10.1016/j.bmc.2025.118535.png)
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Abstract
En 中文
• New pyrazolo[1,5-a]pyrimidine derivatives were synthesized as potential CDK2-targeting anticancer agents. • Compounds 13g, 13j, 21c, and 26b exhibited strong cytotoxicity against HCT-116 colon cancer cells. • Compounds 13g (IC50 = 0.45 μM) and 21c (IC50 = 0.09 μM) were the most potent, with low toxicity toward normal WI-38 fibroblasts. • In vitro CDK2 inhibition assays showed IC50 values of 18–150 nM, with compound 21c being the most active. • 21c induced G1-phase arrest, dual-pathway apoptosis activation, and showed favorable CDK2 binding in docking studies.
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3
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1.7W
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