In this study new 13-amino derivatives of dehydrocostus lactone DHLC (1–4) were synthesized through Michael addition reactions, and were screened against three different breast cancer cell lines, namely hormone receptor positive breast cancer (MCF-7), triple-negative breast cancer (HCC70), and non-tumorigenic mammary epithelial (MCF-12A) cell lines. This evidence concerns the gene NR4A1 and triple-negative breast carcinoma.