4,5-dihydro-1H-thieno [2′,3′:2,3]thiepino[4,5-c]pyrazole-3-carboxamide derivatives were effective against EGFR highly expressing human lung cancer A549 cell line in vitro and the molecular docking procedure revealed the similar EGFR-binding sites and modes of conformation (e.g., MET769) between the most effective derivative and gefitinib, a well-known EGFR inhibitor [40]. This evidence concerns the gene EGFR and lung cancer.