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

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.