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

Fingerprint

Phenanthridines
Type I DNA Topoisomerase
Structure-Activity Relationship
Cytotoxicity
Antineoplastic Agents
Nitrogen
Substitution reactions
cinnoline

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry

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.

Aza-analogs of dibenzo[c,h]cinnoline : Triazachrysenes as potent topoisomerase I-targeting anticancer agents. / Singh, Sudhir K.; Ruchelman, Alexander L.; Zhou, Nai; Li, Tsai Kun; Liu, Angela; Liu, Leroy-Fong; LaVoie, Edmond J.

In: Medicinal Chemistry Research, Vol. 12, No. 1, 2003, p. 1-12.

Research output: Contribution to journalArticle

Singh, SK, Ruchelman, AL, Zhou, N, Li, TK, Liu, A, Liu, L-F & LaVoie, EJ 2003, 'Aza-analogs of dibenzo[c,h]cinnoline: Triazachrysenes as potent topoisomerase I-targeting anticancer agents', Medicinal Chemistry Research, vol. 12, no. 1, pp. 1-12.
Singh, Sudhir K. ; Ruchelman, Alexander L. ; Zhou, Nai ; Li, Tsai Kun ; Liu, Angela ; Liu, Leroy-Fong ; LaVoie, Edmond J. / Aza-analogs of dibenzo[c,h]cinnoline : Triazachrysenes as potent topoisomerase I-targeting anticancer agents. In: Medicinal Chemistry Research. 2003 ; Vol. 12, No. 1. pp. 1-12.
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