Design and synthesis of novel cytotoxic podophyllotoxin derivatives

被引:9
作者
Xi, Wen Li [4 ]
Cai, Qian [4 ]
Tang, Yan Bo [1 ,2 ,3 ]
Sun, Hua [1 ,2 ,3 ]
Xiao, Zhi Yan [1 ,2 ,3 ]
机构
[1] Chinese Acad Med Sci, Key Lab Bioact Subst & Resources Utilizat Chinese, Minist Educ, Beijing 100050, Peoples R China
[2] Chinese Acad Med Sci, Inst Mat Med, Beijing 100050, Peoples R China
[3] Peking Union Med Coll, Beijing 100050, Peoples R China
[4] Liaoning Univ Tradit Chinese Med, Sch Pharm, Dalian 116600, Peoples R China
关键词
Podophyllotoxin; C4-derivation; Cytotoxicity; ANTITUMOR AGENTS; INHIBITORS;
D O I
10.1016/j.cclet.2010.03.040
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
In order to investigate the effect of different C4 linkage moieties on the cytotoxicity of podophyllotoxin derivatives, novel 4-N-and 4-C-substituted 4'-O-demethylepipodophyllotoxin derivatives were designed and synthesized. All the compounds were tested against A549 and MCF-7 tumor cells in vitro, and six compounds showed significant cytotoxicity. The most active compound 9f was superior to GL-331, and exhibited potent cytotoxicity with IC50 value at 10(-7) mol/L level. (C) 2010 Zhi Yan Xiao. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
引用
收藏
页码:1153 / 1156
页数:4
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