A series of novel 5-cyano-2,4,6-substituted pyrimidine derivatives containing acrylamide group were designed, synthesized, and evaluated for their antitumor activity against four human cancer cell lines (MGC-803, PC-3, A549, and H1975) using the MTT assay. Among them, compound 20y exhibited the most potent cytotoxicity against PC-3 cells (IC₅₀ = 2.75 ± 0.08 μM). Notably, compound 20y significantly inhibited the colony formation, migration, and invasion of PC-3 cells. Furthermore, compound 20y induced S-phase cell cycle arrest and apoptosis in PC-3 cells. These findings indicate that compound 20y might serve as a valuable lead compound for developing antitumor agents targeting prostate cancer cells.

Graphical Abstract

中文翻译：

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含丙烯酰胺基的5-氰基-2,4,6-取代嘧啶衍生物的设计、合成及抗肿瘤活性评价

设计、合成了一系列新型含丙烯酰胺基团的 5-氰基-2,4,6-取代嘧啶衍生物，并评估了其对四种人类癌细胞系（MGC-803、PC-3、A549 和 H1975）的抗肿瘤活性。 ）使用MTT测定。其中，化合物20y对PC-3细胞表现出最强的细胞毒性（IC ₅₀  = 2.75 ± 0.08 μM）。值得注意的是，化合物20y显着抑制PC-3细胞的集落形成、迁移和侵袭。此外，化合物20y诱导PC-3细胞中S期细胞周期停滞和细胞凋亡。这些发现表明，化合物20y可能作为一种有价值的先导化合物，用于开发针对前列腺癌细胞的抗肿瘤药物。

图形概要