Aza-analogs of dibenzo[c,h]cinnoline: Triazachrysenes as potent topoisomerase I-targeting anticancer agents

Sudhir K. Singh, Alexander L. Ruchelman, Nai Zhou, Tsai Kun Li, Angela Liu, Leroy-Fong Liu, Edmond J. LaVoie

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

2,3-Dimethoxy-8,9-methylenedioxydibenzo[c,h]cinnoline 1 exhibits greater topoisomerase I (TOP1)-targeting activity and cytotoxicity than its benzo[i]phenanthridine analog. 1,5,6-, 5,6,11-, and 5,6,12-Triazachrysene analogs were prepared to determine the influence of further aza-substitution on TOP1-targeting activity and cytotoxicity. The data reinforce the structure-activity relationships previously observed and indicate that a nitrogen heteroatom can be tolerated at the 11- or 12-position without adversely affecting the TOP1-targeting activity or cytotoxicity of 1.

Original languageEnglish
Pages (from-to)1-12
Number of pages12
JournalMedicinal Chemistry Research
Volume12
Issue number1
Publication statusPublished - 2003
Externally publishedYes

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry

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  • Cite this

    Singh, S. K., Ruchelman, A. L., Zhou, N., Li, T. K., Liu, A., Liu, L-F., & LaVoie, E. J. (2003). Aza-analogs of dibenzo[c,h]cinnoline: Triazachrysenes as potent topoisomerase I-targeting anticancer agents. Medicinal Chemistry Research, 12(1), 1-12.