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Paper | Regular issue | Vol 102, No. 12, 2021, pp.2319-2330
Published online, 7th September, 2021
DOI: 10.3987/COM-21-14526
Synthesis and Biological Evaluation of New Pyrimidine Derivatives as FAK Inhibitors for Development of Antitumor Agents

Di Zhang, Qin Wang, Jing Yang, Qing Zhang, Yi Le, Li Liu, and Longjia Yan*

*School of Pharmaceutical Sciences, Guizhou University, Guiyang 550025, China


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.