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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 F. Liu
  • , Edmond J. LaVoie

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

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
StatePublished - 20 Nov 2003
Externally publishedYes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

  1. SDG 3 - Good Health and Well-being
    SDG 3 Good Health and Well-being

ASJC Scopus subject areas

  • General Pharmacology, Toxicology and Pharmaceutics
  • Organic Chemistry

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