Concise syntheses of N-aryl-5,6,7-trimethoxyindoles as antimitotic and vascular disrupting agents: Application of the copper-mediated Ullmann-type arylation

Hsueh Yun Lee, Jang-Yang Chang, Ling-Yin Chang, Wen-Yang Lai, Mei-Jung Lai, Kuang-Hsing Shih, Ching-Chuan Kuo, Chi-Yen Chang, Jing Ping Liou

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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.

Original languageEnglish
Pages (from-to)3154-3157
Number of pages4
JournalOrganic and Biomolecular Chemistry
Issue number9
Publication statusPublished - May 7 2011


ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Biochemistry

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