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

研究成果: 雜誌貢獻文章

44 引文 斯高帕斯(Scopus)

摘要

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.

原文英語
頁(從 - 到)6412-6415
頁數4
期刊Journal of Medicinal Chemistry
49
發行號21
DOIs
出版狀態已發佈 - 十月 2006

ASJC Scopus subject areas

  • Organic Chemistry

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