Design, synthesis and anti-tumor activity studies of oleanolic acid derivatives using VEGFR as target
10.16438/j.0513-4870.2018-0731
- VernacularTitle:以VEGFR为靶点的齐墩果酸衍生物的设计、合成及抗肿瘤活性研究
- Author:
Yan-ling SONG
1
;
Zhong-yan LIU
1
;
Ling LI
1
;
Jie LI
1
;
Peng-bo ZHANG
1
Author Information
1. Institute of Pharmaceutical and Biological Engineering, Shenyang University of Chemical Technology, Shenyang 110142, China
- Publication Type:ORIGINAL ARTICLES
- Keywords:
oleanolic acid derivative;
synthesis;
molecular docking;
anti-tumor activity
- From:
Acta Pharmaceutica Sinica
2018;53(11):1852-1861
- CountryChina
- Language:Chinese
-
Abstract:
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.
