Synthesis and biological evaluation of noscapine analogues as microtubule-interfering agents.
- Author:
Hou-ling DAI
1
;
Jian-bin ZHENG
;
Min LIN
;
Jing ZHENG
;
Fu-sheng ZHOU
;
Xiao-chun DONG
;
Lei GUO
;
Jian-wen LIU
;
Ren WEN
Author Information
1. School of Pharmacy, East China University of Science and Technology, Shanghai, China.
- Publication Type:Journal Article
- MeSH:
Antineoplastic Agents;
chemical synthesis;
pharmacology;
Cell Cycle;
drug effects;
HL-60 Cells;
Humans;
Noscapine;
analogs & derivatives;
chemical synthesis;
pharmacology;
Polymerization;
drug effects;
Tubulin;
metabolism;
Tubulin Modulators;
chemical synthesis;
pharmacology
- From:
Acta Pharmaceutica Sinica
2012;47(10):1347-1357
- CountryChina
- Language:English
-
Abstract:
A series of noscapine analogues have been synthesized via 13-step reaction starting from 2-hydroxy-3-methoxybenzaldehyde. Anti-tumor activities of these compounds were evaluated against HL-60 cell lines in vitro by the standard MTT assay. It was found that most of these derivatives showed appreciable inhibitory activity against HL-60 and tubulin polymerization. The results also indicated that the potency of compound 31 is about three times more than that ofnoscapine against HL-60 cell line and tubulin polymerization. Moreover, it induced a massive accumulation of cells in G2/M phase. These results showed noscapine and its derivatives were worth to be intensively studied further.
