Synthesis and Cytotoxicity Evaluation of Tropinone Derivatives  

作　　者：Xiu-Juan Yin Chang-An Geng Xing-Long Chen Chang-Li Sun Tong-Hua Yang Tian-Ze Li Jun Zhou Xue-Mei Zhang Ji-Jun Chen 

机构地区：[1]State Key Laboratory of Phytochemistry and Plant Resources in West China,Kunming Iastitute of Botany,Chinese Academy of Sciences,Kunming 650201,China [2]University of Chinese Academy of Sciences,Beijing 100049,China [3]Key Laboratory of Natural Medicinal Chemistry,Kunming Iastitute of Botany,Chinese Academy of Sciences,Kunming 650201,China

出　　处：《Natural Products and Bioprospecting》2017年第2期215-223,共9页应用天然产物（英文）

基　　金：supported by the Hundred Talents Program of the Chinese Academy of Sciences(CAS),the Youth Innovation Promotion Association,CAS and the Program of Yunling Scholarship.

摘　　要：Sixteen tropinone derivatives were prepared,and their antitumor activities against five human cancer cells(HL-60,A-549,SMMC-7721,MCF-7 and SW480)were evaluated with MTS[3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxy methoxyphenyl)-2-(4-sulfopheny)-2H-tetrazolium]assay.Most of the derivatives exhibited better activities compared with tropinone at the concentration of 40 pM.Particularly,derivative 6 showed significant activities with IC50 values of 3.39,13.59,6.65,13.09 and 12.38 pM respectively against HL-60,A-549,SMMC-7721,MCF-7 and SW480 cells,which suggested more potent activities than that of cis-dichlorodiamineplatinum(DDP).

关 键 词：TROPINONE Claisen-Schmidt reaction MTS CYTOTOXICITY 

分 类 号：R73[医药卫生—肿瘤]