Efficient synthesis of panaxadiol derivatives using continuous-flow microreactor and evaluation of anti-tumor activity

被引:20
作者
Wu, Yan [1 ]
Chen, Wei-Qi [2 ]
Zhao, Yu-Qing [3 ]
Piao, Hu-Ri [1 ]
机构
[1] Yanbian Univ, Coll Pharm, Affiliated Minist Educ, Key Lab Nat Resources & Funct Mol Changbai Mt, Yanji 133000, Peoples R China
[2] Fudan Univ, Dept Chem, Shanghai 200433, Peoples R China
[3] Shenyang Pharmaceut Univ, Sch Tradit Chinese Mat Med, Shenyang 110016, Peoples R China
基金
中国国家自然科学基金;
关键词
Flow chemistry; Microreactor; Panaxadiol; Anti-tumor activity; KOREAN GINSENG; CHEMISTRY; CELLS; SYSTEM;
D O I
10.1016/j.cclet.2014.11.013
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
An efficient method has been developed for the synthesis of a series of (20R)-panaxadiol derivatives (4a-w) using a continuous-flow microreactor. The antitumor activities of the newly synthesized compounds were evaluated in vitro in two human prostate adenocarcinoma tumor cell lines (i.e., PC-3 and LNCaP cells), and their cytotoxicities were evaluated using a standard Ma assay. Compounds 4c, 4h, 4p, 4q and 4s exhibited higher antitumor activities toward PC-3 cell line than panaxadiol, which was used as a reference standard. (C) 2014 Yu-Qing Zhao and Hu-Ri Piao. Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. All rights reserved.
引用
收藏
页码:334 / 338
页数:5
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