Three compounds, 2b, 2f, and 2i, exhibited the most potent activity (GI50: 4.03, 2.94, and 2.96 μM, respectively) and the best tumor selectivity (ratio: more than 7.44) against the MDA-MB-468 cell line as an EGFR-overexpressed TNBC. The gene discussed is EGFR; the disease is neoplasm.