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Short Paper | Regular issue | Vol 104, No. 3, 2022, pp.556-572
Published online, 22nd December, 2021
DOI: 10.3987/COM-21-14594
Development of 5-Trifluoromethylpyrimidine Derivatives as Dual Inhibitors of EGFR and Src for Cancer Therapy

Qin Wang, Nian Rao, Li Liu,* Yi Le, and Longjia Yan*

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


In this paper, we reported a new series of 5-trifluoromethylpyrimidine derivatives (4a-4f, 6a-6j) for cancer therapy. They were tested for antitumor activity in vitro on four human cancer cell lines including A549, K562, HepG2, MCF-7 and two kinase including wild type epidermal growth factor receptor tyrosine kinase (EGFRwt-TK) and c-Src. The results suggested that some of the compounds (4a, 4b, 4c, 4e, 6b, 6d, 6e, 6f, 6g, 6h) performed well activities. Especially 2-((2-((4-((2-(cyclohexylamino)-3,4-dioxocyclobut-1-en-1-yl)aminophenyl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)-N-methylbenzamide (6g) showed high antitumor activities against four cancer cell lines with 1.08 μM, 2.06 μM, 1.24 μM and 2.57 μM, respectively. Furthermore, compound 6g inhibited EGFRwt and Src at the values of 0.75 μM and 0.15 μM.