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

研究成果: 雜誌貢獻文章同行評審

6 引文 斯高帕斯(Scopus)

摘要

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.

原文英語
頁(從 - 到)1-12
頁數12
期刊Medicinal Chemistry Research
12
發行號1
出版狀態已發佈 - 2003
對外發佈Yes

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry

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