Concise syntheses of N-aryl-5,6,7-trimethoxyindoles as antimitotic and vascular disrupting agents: application of the copper-mediated Ullmann-type arylation
Concise syntheses of N-aryl-5,6,7-trimethoxyindoles as antimitotic and vascular disrupting agents: application of the copper-mediated Ullmann-type arylation
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DOI：
10.1039/c0ob01038c
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发表时间：
2011-01-01
影响因子：
3.2
通讯作者：
Liou, Jing-Ping
中科院分区：
文献类型：
--
作者：
Lee, Hsueh-Yun;Chang, Jang-Yang;Liou, Jing-Ping
为了模拟考布他汀A-4的3，4，5-三甲氧基苯基-Z-二苯乙烯部分，通过相应的5，6，7-三甲氧基吲哚和芳基卤化物通过铜催化的Ullmann型N-芳基化反应合成了一系列N-芳基-5，6，7-三甲氧基吲哚。这些合成的化合物显示出有效的抗增殖活性，为有效的微管蛋白聚合抑制剂提供了新的骨架。
In an attempt to mimic the 3,4,5-trimethoxyphenyl-Z-stilbene moiety of combretastatin A-4, a series of N-aryl-5,6,7-trimethoxyindoles were synthesized via copper-catalyzed Ullmann-type N-arylation through the corresponding 5,6,7-trimethoxyindole and aryl halides. These synthesized compounds demonstrated potent antiproliferative activity providing a novel skeleton for potent tubulin polymerization inhibitors.