A new series of pyrimidine derivatives containing aryl urea moieties was designed and synthesized. The anticancer activities of all compounds were evaluated in vitro against colon and prostat cancer cell lines by MTT assay. Among these compounds, 4b exhibited the highest cytotoxic activity against SW480 cancer cell line with IC₅₀ value of 11.08 µM. Mechanistic studies showed that compound 4b arrested cell cycle at G2/M phase and induced apoptosis through upregulating Bax, Ikb-α and cleaved PARP and downregulating Bcl-2 expression levels. Moreover, compound 4b induced loss of mitochondrial membrane potential in SW480 cells. These results suggest that pyrimidine with urea moieties could be a template for designing new anticancer agents.

设计并合成了一系列新的含芳基脲部分的嘧啶衍生物。通过MTT分析在体外评估了所有化合物的抗癌活性。在这些化合物中，4b对SW480癌细胞系表现出最高的细胞毒活性，IC ₅₀值为11.08 µM。机理研究表明，化合物4b通过上调Bax，Ikb-α和裂解PARP以及下调Bcl-2表达水平，在G2 / M期阻止细胞周期并诱导凋亡。此外，化合物4b诱导SW480细胞线粒体膜电位的损失。这些结果表明，具有尿素部分的嘧啶可能是设计新抗癌药的模板。