2-Amino and 2′-aminocombretastatin derivatives as potent antimitotic agents

Jang Yang Chang, Ming Fang Yang, Chi Yen Chang, Chi Ming Chen, Ching Chuan Kuo, Jing Ping Liou

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Abstract

A novel series of 2-amino and 2′-aminocombretastatin derivatives were synthesized and evaluated for antitumor activity. Several compounds had excellent antiproliferative activity as inhibitors of tubulin polymerization. Compounds 11, 20, and 21 with IC50 values of 1.6, 1.7, and 1.8 μM, respectively, exhibited more potent inhibition of tubulin polymerization than colchicine and approximately as active as combretastatin A-4. They also displayed antiproliferative activity with an IC50 values ranging from 11 to 44 nM in a variety of human cell lines from different organs. Structure activity relationship information suggests that the NH2 substituent at the 2-position of either ring A or ring B in combretastatin molecular skeleton may play an important role in the bioactivity of this series of compounds.

Original languageEnglish
Pages (from-to)6412-6415
Number of pages4
JournalJournal of Medicinal Chemistry
Volume49
Issue number21
DOIs
Publication statusPublished - Oct 2006

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ASJC Scopus subject areas

  • Organic Chemistry

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