Synthesis and cytotoxicity of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives bearing 3,4,5-trimethoxyphenyl moiety

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• 作者：Pei-Liang Zhao ; An-Na Duan ; Min Zou ; Hai-Kui Yang ; Wen-Wei You ; ^{youww@smu.edu.cn} ; Shu-Guang Wu ; ^{shuguang@smu.edu.cn}
• 关键词：5 ; 6-Dihydro-[1 ; 2 ; 4]triazolo[3 ; 4-b][1 ; 3 ; 4]thiadiazole ; Synthesis ; Antitumor activity
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 July, 2012
• 卷：22
• 期：13
• 页码：4471-4474
• 文件大小：467 K

摘要

A series of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and some novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles bearing 3,4,5-trimethoxyphenyl moiety were synthesized and screened for their anticancer activity. The preliminary bioassay results indicated that compounds 14 and 16 showed much stronger cytotoxicity than Doxorubicin against HepG2 cell lines with IC₅₀ values of 0.58 and 3.17 渭M, respectively. Meanwhile compound 16 also exhibited a broad spectrum of antitumor activity against MCF-7 and MKN45 with IC₅₀ values of 10.92 and 13.79 渭M, respectively.