Design, synthesis, and biological evaluation of novel alkylsulfanyl-1,2,4-triazoles as cis-restricted combretastatin A-4 analogues

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• 作者：Yan-Hong Li¹ ; Bei Zhang¹ ; Hai-Kui Yang ; Qiu Li ; Peng-Cheng Diao ; Wen-Wei You ; ^{youww@smu.edu.cn} ; Pei-Liang Zhao ; ^{plzhao@smu.edu.cn}
• 关键词：Alkylsulfanyl-1 ; 2 ; 4-triazoles ; Synthesis ; Antiproliferative activity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：1098-1106
• 全文大小：979 K
• 卷排序：125

文摘

32 novel 1,2,4-triazole derivatives were designed and synthesized as cis-restricted combretastatin A-4 analogues. Antiproliferative activity of these compounds was evaluated. Analogues 20 and 25 exhibited much stronger antitumor activity than CA-4. Flow-activated cell sorting analysis suggested that compound 20 mainly arrested PC-3 cells in G2/M stage.