In summary, new 13-amino derivatives of dehydrocostus lactone (1–4) were synthesized through Michael’s addition reactions and were screened against breast cancer cell lines including hormone receptor-positive breast cancer (MCF-7), triple-negative breast cancer (HCC70), and non-tumorigenic mammary epithelial (MCF-12A) cell lines. The gene discussed is NR4A1; the disease is breast carcinoma.