Design, synthesis and anticancer activity studies of oleanolic acidderivatives targeting mTOR
10.16438/j.0513-4870.2018-0890
- VernacularTitle:以mTOR激酶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
;
Ling LI
1
;
Zhong-yan LIU
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:Research Article
- Keywords:
oleanolic acid derivative;
synthesis;
molecular docking;
anti-tumor activity
- From:
Acta Pharmaceutica Sinica
2019;54(2):335-342
- CountryChina
- Language:Chinese
-
Abstract:
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.
