Synthesis and structure-activity relationship of cycloberberine as anti-cancer agent.
- Author:
Chongwen BI
;
Caixia ZHANG
;
Yangbiao LI
;
Wuli ZHAO
;
Rongguang SHAO
;
Lin MEI
;
Danqing SONG
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2013;48(12):1800-6
- CountryChina
- Language:Chinese
-
Abstract:
A series of cycloberberine derivatives were designed, synthesized and evaluated for their anti-cancer activities in vitro. Among these analogs, compounds 6c, 6e and 6g showed strong inhibition on human HepG2 cells. They afforded a potent effect against DOX-resistant MCF-7 breast cells as well. The primary mechanism showed that cell cycle was blocked at G2/M phase of HepG2 cells treated with 6g using flow cytometry assay. It significantly inhibited the activity of DNA Top I at the concentration of 0.1 mg mL-1. Our results provided a basis for the development of this kind of compounds as novel anti-cancer agents.
