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

Research output: Contribution to journalArticle

11 Citations (Scopus)


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.

Original languageEnglish
Pages (from-to)7824-7831
Number of pages8
JournalBioorganic and Medicinal Chemistry
Issue number16
Publication statusPublished - Aug 15 2008
Externally publishedYes



  • Antitumor
  • Athymic mice
  • Cinnolines
  • Cytotoxicity
  • Human tumor xenografts
  • Isoquino[4,3-c]cinnolin-12-ones
  • Multidrug resistance
  • Topoisomerase

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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