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

研究成果: Article同行評審

13 引文 斯高帕斯(Scopus)

摘要

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).

原文English
頁(從 - 到)588-593
頁數6
期刊ChemMedChem
4
發行號4
DOIs
出版狀態Published - 2009 四月 17

All Science Journal Classification (ASJC) codes

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

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