Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Angiogenesis Inhibitors / chemical synthesis*
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Angiogenesis Inhibitors / pharmacology
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Antimitotic Agents / chemical synthesis*
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Antimitotic Agents / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Copper / chemistry*
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Humans
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Indoles / chemical synthesis*
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Indoles / pharmacology
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Molecular Structure
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Structure-Activity Relationship
Substances
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Angiogenesis Inhibitors
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Antimitotic Agents
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Indoles
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Copper