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

    Yan Wua,1, Wei-Qi Chenb,1, Yu-Qing Zhaoc, Hu-Ri Piaoa

    • 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.

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