EGFR and neoplasm: The most promising was 161 with R3 = Et, R4 = Ph, and R5 = H, revealing potent EGFR inhibitory activity [IC50 = 5.2, 9.6, and 1.9 nM, against EGFR(WT), EGFR(d746-750), and EGFR(L858R), respectively], antiproliferation properties (IC50 = 4.1, 0.5, and 2.1 μM against A549, PC-9, and A431, respectively), arresting the cell cycle at the G0/G1 phases (flow cytometry), and apoptosis induction, in addition to tumor growth suppression evidenced by in vivo testing (BALB/c nude mouse model, oral administration) [163].