THE SYNTHESIS, ANTITUMOR ACTIVITY, AND SAR OF N-SUBSTITUTED γ-AMINOPROPYLSILATRANE DERIVATIVES

被引:9
|
作者
Guo Ping [1 ]
Wang Yue-Wu [1 ]
Luo Xin-Tong [1 ]
Qi Xiao-Lu [1 ]
Hou Le-Ping [1 ]
Xie Zi-Xin [1 ]
Ye Fa-Qing [1 ]
机构
[1] Wenzhou Med Coll, Sch Pharm, Wenzhou 325035, Zhejiang, Peoples R China
关键词
-Aminopropylsilatrane derivatives; structure-activity relationship (SAR); physiological activity; SILATRANES; GERMATRANES;
D O I
10.1080/10426507.2013.829835
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
-Aminopropylsilatrane has been reported to possess biological activity against tumor cancer cells with low cytotoxicity in many kinds of silatranes. So some N-substituted -aminopropylsilatrane derivatives were synthesized and assayed by a primary anticancer screening against HT-29, Hela, and MDAMB435 cells by the use of the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) method. The structures of these derivatives were confirmed by H-1 NMR, electrospray ionization-mass spectrometry, and elemental analysis. The structure-activity relationship showed that the N-substituted derivatives exhibit better activity in which the -amino group of the silatrane is connected with stronger electron-withdrawing groups.
引用
收藏
页码:511 / 518
页数:8
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