In this paper, a set of new pyrimidine derivatives was designed and synthesized. Subsequently, all the final targets were evaluated for antitumor activities in vitro on four human cancer cell lines including U-87 MG, MDA-MB-231, PC-3, and MCF-7, which were high expressed with focal adhesion kinase (FAK). The results were shown that these compounds performed well antitumor activities. Especially 2-((2-((4-((2-((2-acrylamidoethyl)amino)-3,4-dioxocyclobut-1-en-1-yl)amino)phenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-N-methylbenzamide (7b) exhibited the highest antitumor activities with 2.16 μM, 2.03 μM, 6.19 μM, and 21.31 μM, respectively. In addition, all the compounds were tested activities against FAK and compound 7b was also the best candidate with IC50 value of 5.9 nM.

中文翻译：

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新型嘧啶衍生物作为 FAK 抑制剂的合成和生物学评价，用于开发抗肿瘤剂

本文设计并合成了一组新的嘧啶衍生物。随后，在体外评估了所有最终靶标对四种人癌细胞系的抗肿瘤活性，包括 U-87 MG、MDA-MB-231、PC-3 和 MCF-7，这些细胞系与粘着斑激酶 (FAK) 高表达）。结果表明，这些化合物具有良好的抗肿瘤活性。特别是2-(((2-((4-((2-((2-丙烯酰胺乙基)氨基)-3,4-二氧代环丁-1-烯-1-基)氨基)苯基)氨基)-5-(三氟甲基) pyrimidin-4-yl)amino) -N - methylbenzamide ( 7b ) 表现出最高的抗肿瘤活性，分别为 2.16 μM、2.03 μM、6.19 μM 和 21.31 μM。此外，测试了所有化合物对 FAK 和化合物的活性7b也是最佳候选，IC 50值为5.9 nM。