Synthesis and structure-activity relationship of 2-aminobenzophenone derivatives as antimitotic agents

Jing Ping Liou, Chun Wei Chang, Jeng Shin Song, Yung Ning Yang, Ching Fang Yeh, Huan Yi Tseng, Yu Kang Lo, Yi Ling Chang, Chung Ming Chang, Hsing Pang Hsieh

研究成果: 雜誌貢獻文章同行評審

133 引文 斯高帕斯(Scopus)

摘要

A new type of inhibitor of tubulin polymerization was discovered on the basis of the combretastatin molecular skeleton. The lead compounds in this series, compounds 6 and 7, strongly inhibited tubulin polymerization in vitro and significantly arrested cells at the G2/M phase. Compounds 6 and 7 yielded 50- to 100-fold lower IC50 values than did combretastatin A-4 against Colo 205, NUGC3, and HA22T human cancer cell lines as well as similar or greater growth inhibitory activities than did combretastain A-4 against DLD-1, HR, MCF-7, DU145, HONE-1, and MES-SA/DX5 human cancer cell lines. Structure-activity relationship information revealed that introduction of an amino group at the ortho position of the benzophenone ring plays an integral role for increased growth inhibition.

原文英語
頁(從 - 到)2556-2562
頁數7
期刊Journal of Medicinal Chemistry
45
發行號12
DOIs
出版狀態已發佈 - 6月 6 2002
對外發佈

ASJC Scopus subject areas

  • 有機化學

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