Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity

Alexander L. Ruchelman, Shejin Zhu, Nai Zhou, Angela Liu, Leroy-Fong Liu, Edmond J. LaVoie

Research output: Contribution to journalArticle

17 Citations (Scopus)


The exceptional TOP1-targeting activity and antitumor activity of ARC-111, 1, prompted studies on similarly substituted benzo[i]phenanthridine-12- carboxylic ester and amide derivatives. These studies were extended to include 6-substituted 8,9-dimethoxy-2,3-methylenedioxy-dibenzo[c,h][2,6]naphthyridin-5- ones, which represent reversed lactam analogues of 1. Several of these analogues retained the potent TOP1-targeting activity and cytotoxicity observed for ARC-111.

Original languageEnglish
Pages (from-to)5585-5589
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Issue number22
Publication statusPublished - Nov 15 2004
Externally publishedYes



  • Anticancer
  • Benzo[i]phenanthridines
  • Cytotoxic agents
  • Dibenzo[c,h]naphthyridines
  • Topoisomerase I

ASJC Scopus subject areas

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

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