Design, synthesis and anticancer activity studies of oleanolic acidderivatives targeting mTOR / 药学学报

Ten novel oleanolic acid (OA) derivatives containing urea or thiourea group were designed and synthesized, the chemical structures were confirmed by 1H NMR, 13C NMR and HR-MS. All of these compounds were evaluated for the inhibitory activity against growth of HepG2 and SGC7901 cells. The results showed that compounds I3 and II3 exhibited significant antitumor activities with IC50 of 9.4 and 5.5 μmol·L-1, respectively. Molecular docking studies showed that all these compounds exhibit inhibitory ability against mTOR kinase. Compounds I3 and II3 were further evaluated for the inhibitory activity against mTOR kinase. The results showed that I3 and II3 exhibited strong inhibitory effect on mTOR kinase with IC50 values of 0.83 and 0.26 μmol·L-1.

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

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.