Design, synthesis and anti-tumor activity of oleanolic acid derivatives targeting EGFR

With computer-aided drug design (CADD) technology, a total of 12 inhibitors of EGFR based on oleanolic acid (OA) derivatives were designed and synthesized with modification at C-3 and C-28 positions of OA. Their structures were confirmed by ¹H-NMR,¹³C-NMR and ESI-MS. The anti-tumor activities of these novel analogues were evaluated by MTT assay, and the results showed that the derivatives I₆ and II₂ had stronger cytotoxicity on A549 and MCF-7 cancer cells, which may be potential candidate compounds for tumor therapy.