A series of novel pteridinone derivatives possessing a hydrazone moiety were designed, synthesized and evaluated for their biological activity. Most of the synthesized compounds demonstrated moderate to excellent activity against A549, HCT116 and PC-3 cancer cell lines. In particular, compound L₁₉ exhibited the most potent antiproliferative effects on three cell lines with IC₅₀ values of 3.23 μM, 4.36 μM and 8.20 μM, respectively. In kinase assays, the compound L₁₉ also showed potent inhibition activity toward PLK1 with % inhibition values of 75.1. Further mechanism studies revealed that compound L₁₉ significantly inhibited proliferation of HCT-116 cell lines, induced a great decrease in mitochondrial membrane potential resulting in apoptosis of cancer cells, inhibited the migration of tumor cells, and arrested G1 phase of HCT116 cells.

设计、合成了一系列具有腙部分的新型蝶啶酮衍生物并评估了其生物活性。大多数合成的化合物对 A549、HCT116 和 PC-3 癌细胞系表现出中等至优异的活性。特别是，化合物L ₁₉对三种细胞系表现出最有效的抗增殖作用，IC ₅₀值分别为3.23 μM、4.36 μM和8.20 μM。在激酶测定中，化合物L ₁₉还显示出对 PLK1 的有效抑制活性，抑制百分比值为 75.1。进一步的机制研究表明，化合物L ₁₉显着抑制HCT-116细胞系的增殖，诱导线粒体膜电位大幅下降导致癌细胞凋亡，抑制肿瘤细胞的迁移，并阻滞HCT116细胞的G1期。