Synthesis and antitumor activity of 13-acylmatrine derivatives
10.3969/j.issn.1006-0111.2017.01.004
- VernacularTitle:13-酰胺基取代苦参碱衍生物的合成及抗肿瘤活性研究
- Author:
Ben FU
1
;
Yuntao TIAN
;
Li DING
;
Qiuye WU
;
Zhongwu GUO
;
Qingjie ZHAO
Author Information
1. 第二军医大学药学院有机化学教研室
- Keywords:
matrine;
derivatives;
synthesis;
antitumor activity
- From:
Journal of Pharmaceutical Practice
2017;35(1):12-16
- CountryChina
- Language:Chinese
-
Abstract:
Objective To synthesize a series of 13-acylmatrine derivatives and evaluate their in vitro antitumor activity . Methods Using sophocarpine as the starting material ,a series of new compounds were synthesized through Michael addition , Staudinger reduction and acylation .The structure of target compounds were confirmed by 1 H NMR and MS techniques .Their antitumoractivityagainsthumanhepatomacells(BEL-7404)andmicemelanomacells(K111)wereevaluated invitrobyMTT assay .Results We synthesized 9 compounds and all the compounds exhibited inhibitory activities against BEL-7404 and K111 . Conclusion Compound 4b and compound 4e exhibit good in vitro antitumor activity to human hepatoma cells (BEL-7404) .