Design, synthesis and anti-tumor activity studies of oleanolic acid derivatives using VEGFR as target

In this study, twenty containing ethylenediamine groups derivatives of oleanolic acid (OA) were synthesized, their structures were determined by ¹H NMR, ¹³C NMR and HR-MS. The anti-tumor activities in HepG2 and SGC7901 cells were evaluated by MTT assay. The results showed that all compounds exhibited anti-tumor activity, compounds I₆, I₈ and I₉ exhibited significant anti-tumor activities with IC₅₀ values of 16.7, 9.8 and 6.3 μmol·L^-1, respectively. Molecular docking studies showed that compounds I₆-I₉ produce higher combining ability with VEGFR. Compound I₆-I₉ were further evaluated for the inhibitory activity against VEGFR-2, the result showed I₉ had a strong inhibitory effect on VEGFR with IC₅₀ values of 0.56 μmol·L^-1.