Among these compounds, compound 41 not only exhibited high inhibitory activity of FAK kinase (IC50 = 1.03 nM) and EGFR T790M (IC50 = 3.89 nM) but also displayed excellent antiproliferative activity against AsPC-1, BxPC-3, Panc-1 three FAK-overexpressing pancreatic cancer cells (IC50 = 0.909, 0.761, 1.218 μM, respectively) and two drug-resistant cancer cell lines MCF-7/ADR and H1975 cells (IC50 = 0.909, 0.761, 1.218 μM, respectively), which were significantly lower than that of the lead compound TAE-226. The gene discussed is PTK2; the disease is cancer.