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

16 Citations (Scopus)

Abstract

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
Volume14
Issue number22
DOIs
Publication statusPublished - Nov 15 2004
Externally publishedYes

Fingerprint

Type I DNA Topoisomerase
Cytotoxicity
Phenanthridines
Derivatives
Lactams
Amides
Esters
dimethoxybenzo(i)phenanthridine-12-carboxylic acid
topovale

Keywords

  • 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

Cite this

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

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 22, 15.11.2004, p. 5585-5589.

Research output: Contribution to journalArticle

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AU - Ruchelman, Alexander L.

AU - Zhu, Shejin

AU - Zhou, Nai

AU - Liu, Angela

AU - Liu, Leroy-Fong

AU - LaVoie, Edmond J.

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