Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 15, Issue 23, Pages 5154-5159Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.08.056
Keywords
tubulin inhibitor; tubulin polymerization; 1,2,4-triazole; vascular disrupting agent; tumor vasculature; antimitotic
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A novel triazole-containing chemical series was shown to inhibit tubulin polymerization and cause cell cycle arrest in A431 cancer cells with EC50 values in the single digit nanomolar range. Binding experiments demonstrated that representative active compounds of this class compete with colchicine for its binding site on tubulin. The syntheses and structure-activity relationship studies for the triazole derivatives are described herein. (c) 2005 Elsevier Ltd. All rights reserved.
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