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Synthesis and Structure–Activity Relationships of 1‐Benzyl‐4,5,6‐trimethoxyindoles as a Novel Class of Potent Antimitotic Agents
Authors:Mei‐Jung Lai  Ching‐Chuan Kuo Dr  Teng‐Kuang Yeh Dr  Hsing‐Pang Hsieh Dr  Li‐Tzong Chen Dr  Wen‐Yu Pan  Kuang‐Yang Hsu Dr  Jang‐Yang Chang Dr  Jing‐Ping Liou Dr
Affiliation:1. College of Pharmacy, Taipei Medical University, 250 Wu‐Xin Street, Taipei 110 (Taiwan, Republic of China), Fax: (+866)?2‐2736‐1661;2. National Institute of Cancer Research, National Health Research Institutes, Tainan 704 (Taiwan, Republic of China), Fax: (+866)?6‐208‐3427;3. Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35 Keyan Rd., Zhunan Town, Miaoli County 350 (Taiwan, Republic of China);4. Division of Hematology/Oncology, Department of Internal Medicine, National Cheng Kung University Hospital, Tainan 704 (Taiwan, Republic of China)
Abstract:Combretastatin A‐4 derivatives : A series of combretastatin A‐4‐derived 1‐benzyl‐4,5,6‐trimethoxyindoles was designed and prepared as a novel class of potent antimitotic agents acting through the colchicine binding site on the microtubule.
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Keywords:antitumor agents  drug design  inhibitors  structure–  activity relationships  tubulin polymerization
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