We have synthesized four PAMAM conjugates, G4P, G4F, G4L, and G4PFL, and studied their efficiency in anticancer therapy against ER-positive and EGFR-positive A549 non-small-cell lung cancer and U-118 MG glioma cells, and comparatively with ER-positive and EGFR-positive immortalized, non-cancerous human keratinocytes (HaCaT). The gene discussed is ESR1; the disease is central nervous system cancer.