Yan, Longjia; Wang, Qin; Liu, Li; Le, Yi published the artcile< Design, synthesis and biological evaluation of a series of dianilinopyrimidines as EGFR inhibitors>, Application of C19H34O2, the main research area is anilino trifluoromethyl pyrimidinyl thiophenamide preparation EGFR inhibition antitumor pharmacokinetics; Design; EGFR; antitumor; inhibitor; synthesis.
This paper described our efforts to develop dianilinopyrimidines as novel EGFR inhibitors. All the target compounds were tested for inhibitory effects against wild type EGFR (EGFRwt) and three tumor cells, including A549, PC-3, and HepG2. Some of the compounds performed well in antitumor activities. Especially, compound 2-((2-((4-(3-fluorobenzamido)phenyl)amino)-5-(trifluoromethyl) pyrimidin-4-yl)amino)-N-methylthiophene-3-carboxamide showed higher anti-tumor activities than Gefitinib. The IC50 values of compound 2-((2-((4-(3-fluorobenzamido)phenyl)amino)-5-(trifluoromethyl) pyrimidin-4-yl)amino)-N-methylthiophene-3-carboxamide against A549, PC-3, and HepG2. reached 0.56 μM, 2.46 μM, and 2.21 μM, resp. In addition, further studies indicated that compound 2-((2-((4-(3-fluorobenzamido)phenyl)amino)-5-(trifluoromethyl) pyrimidin-4-yl)amino)-N-methylthiophene-3-carboxamide could induce apoptosis against A549 cells and arrest A549 cells in the G2/M phase. Mol. docking studies showed that compound 2-((2-((4-(3-fluorobenzamido)phenyl)amino)-5-(trifluoromethyl) pyrimidin-4-yl)amino)-N-methylthiophene-3-carboxamidecould closely interact with EGFR. Generally, compound 2-((2-((4-(3-fluorobenzamido)phenyl)amino)-5-(trifluoromethyl) pyrimidin-4-yl)amino)-N-methylthiophene-3-carboxamide was the potential for developing into an anti-tumor drug.
Journal of Enzyme Inhibition and Medicinal Chemistry published new progress about Antitumor agents. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Application of C19H34O2.
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