Syntheses and biological evaluation of topoisomerase I-targeting agents related to 11-[2-(N,N-dimethylamino)ethyl]-2,3-dimethoxy-8,9-methylenedioxy-11H-isoquino[4,3-c]cinnolin-12-one (ARC-31)

Mavurapu Satyanarayana, Wei Feng, Liang Cheng, Angela A. Liu, Yuan Chin Tsai, Leroy F. Liu, Edmond J. LaVoie

研究成果: 雜誌貢獻文章同行評審

15 引文 斯高帕斯(Scopus)

摘要

Several 11-ethyl-2,3-dimethoxy-8,9-methylenedioxy-11H-isoquino[4,3-c]cinnolin-12-ones with varied functionality on the ethyl substituent have exhibited potent topoisomerase I (TOP1) targeting activity and antitumor activity. The influence of various polar substituents at the 2-position of the 11-ethyl substituent, including N-methylamine, N-isopropylamine, hydroxyl, and hydroxylamino groups, on TOP1-targeting activity and cytotoxicity was assessed. The N-methylamine and N-isopropylamine derivatives were also evaluated as antitumor agents in athymic nude mice with MDA-MB-435 human tumor xenografts. Both compounds were active as antitumor agents upon either parenteral or oral administration.
原文英語
頁(從 - 到)7824-7831
頁數8
期刊Bioorganic and Medicinal Chemistry
16
發行號16
DOIs
出版狀態已發佈 - 8月 15 2008
對外發佈

ASJC Scopus subject areas

  • 生物化學
  • 分子生物學
  • 有機化學
  • 藥物發現
  • 藥學科學

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