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Efficient synthesis of panaxadiol derivatives using continuous-flow microreactor and evaluation of anti-tumor activity
Authors:Yan Wu  Wei-Qi Chen  Yu-Qing Zhao  Hu-Ri Piao
Affiliation:a Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133000, China;b Department of Chemistry, Fudan University, Shanghai 200433, China;c School of Traditional Chinese Materia Medica, Shenyang Pharmaceutical University, Shenyang 110016, China
Abstract: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.
Keywords:Flow chemistry  Microreactor  Panaxadiol  Anti-tumor activity
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