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

Yan Wu^a,1, Wei-Qi Chen^b,1, Yu-Qing Zhao^c, Hu-Ri Piao^a

• ^aKey Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, China
• ^bDepartment of Chemistry, Fudan University, Shanghai, China
• ^cSchool of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang, China

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 MTT 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.

Read the publication that featured this abstract