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 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).

原文英語
頁(從 - 到)588-593
頁數6
期刊ChemMedChem
4
發行號4
DOIs
出版狀態已發佈 - 4月 17 2009

ASJC Scopus subject areas

  • 藥理學、毒理學和藥劑學 (全部)
  • 有機化學
  • 分子醫學

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