Antitumor Agents. 111.† New 4-Hydroxylated and 4-Halogenated Anilino Derivatives of 4'-Demethylepipodophyllotoxin as Potent Inhibitors of Human DNA Topoisomerase II

Kuo Hsiung Lee, Scott A. Beers, Masami Mori, Zhe Qing Wang, Yao Haur Kuo, Li Li, Su Ying Liu, Jang Yang Chang, Fu Sheng Han, Yung Chi Cheng

研究成果: Article同行評審

111 引文 斯高帕斯(Scopus)

摘要

A series of C-4 hydroxylated and halogenated anilino derivatives of epipodophyllotoxin or 4'-demethylepipodophyllotoxin have been synthesized and evaluated for their inhibitory activity against the human DNA topoisomerase II as well as for their activity in causing cellular protein-linked DNA breakage. Compounds 11-17 and 22 are more potent than etoposide in causing DNA breakage, while compounds 11-13, 15, 16, and 20 are as active or more active than etoposide in their inhibition of the human DNA topoisomerase II. The cytotoxicity in KB cells appears to have no direct correlation with their ability to inhibit DNA topoisomerase II and to cause protein-linked DNA breaks in cells.

原文English
頁(從 - 到)1364-1368
頁數5
期刊Journal of Medicinal Chemistry
33
發行號5
DOIs
出版狀態Published - 1990 5月

All Science Journal Classification (ASJC) codes

  • 分子醫學
  • 藥物發現

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