Synthesis and structure-activity relationships of 1-benzyl-4,5,6- trimethoxyindoles as a novel class of potent antimitotic agents

Mei-Jung Lai, Ching-Chuan Kuo, Teng-Kuang Yeh, Hsing-Pang Hsieh, Li-Tzong Chen, Wen-Yu Pan, Kuang Yang Hsu, Jang-Yang Chang, Jing Ping Liou

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13 Citations (Scopus)

Abstract

A series of 1-benzyl-4,5,6-trimethoxyindoles was designed and prepared as a novel class of potent antimitotic agents acting through the colchicine binding site of tubulin. Compounds 10 and 11 showed excellent antiproliferative activity with mean IC50 values of 26 and 27 n M, respectively, in a diverse set of human cancer lines from different organs, including a MDR+ line. They also displayed substantial antitubulin efficacy with IC50 values of 3.5 and 2.6 μM, respectively, representing an improvement over colchicine (IG50=4.3μM).

Original languageEnglish
Pages (from-to)588-593
Number of pages6
JournalChemMedChem
Volume4
Issue number4
DOIs
Publication statusPublished - Apr 17 2009

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Keywords

  • Antitumor agents
  • Drug design
  • Inhibitors
  • Structure-activity relationships
  • Tubulin polymerization

ASJC Scopus subject areas

  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry
  • Molecular Medicine

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