In an attempt to enhance cytotoxic activity of pyrazolo[3,4-d]pyrimidine core, we synthesized (3,5-dimethylpyrazol-1-yl)-[4-(1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)phenyl]methanone (4) by reacting 4-(1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)benzohydrazide (3) with acetylacetone. Antiproliferative activity of this compound was screened against breast (MCF-7), colon (HCT-116), and liver (HEPG-2) cancer cell lines. The tested compound exhibited cytotoxic activity with IC50 = 5.00–32.52 μM. Moreover, inhibitory activity of this compound was evaluated against the epidermal growth factor receptor (EGFR), the fibroblast growth factor receptor (FGFR), the insulin receptor (IR), and the vascular endothelial growth factor receptor (VEGFR). This target compound showed potent inhibitory activity, especially against FGFR with IC50 = 5.18 μM.

中文翻译：

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（3,5-二甲基吡唑-1-基）-[4-（1-苯基-1H-吡唑并[3,4-d]嘧啶-4-基氨基）苯基]甲酮

为了增强吡唑并[​​3,4-d]嘧啶核的细胞毒性，我们合成了（3,5-二甲基吡唑-1-基）-[4-（1-苯基-1H-吡唑并[3,4-d]通过使4-（1-苯基-1H-吡唑并[3,4-d]嘧啶-4-基氨基）苯甲酰肼（3）与乙酰丙酮反应来制备]嘧啶-4-基氨基）苯基]甲酮（4）。筛选了针对乳腺癌（MCF-7），结肠癌（HCT-116）和肝癌（HEPG-2）癌细胞系的该化合物的抗增殖活性。被测化合物表现出细胞毒活性，IC50 = 5.00–32.52μM。此外，评估了该化合物对表皮生长因子受体（EGFR），成纤维细胞生长因子受体（FGFR），胰岛素受体（IR）和血管内皮生长因子受体（VEGFR）的抑制活性。该目标化合物显示出强大的抑制活性，尤其是针对FGFR的抑制活性，IC50 = 5.18μM。