Diaza- and triazachrysenes: Potent topoisomerase-targeting agents with exceptional antitumor activity against the human tumor xenograft, MDA-MB-435

Alexander L. Ruchelman, Sudhir K. Singh, Xiaohua Wu, Abhijit Ray, Jin Ming Yang, Tsai Kun Li, Angela Liu, Leroy-Fong Liu, Edmond J. LaVoie

研究成果: 雜誌貢獻文章

49 引文 斯高帕斯(Scopus)

摘要

Several 5,12-diazachrysen-6-ones and 5,6,11-triazachrysen-12-ones were synthesized with varied substituents at the 5- or 11-position, respectively. Each compound was evaluated for its potential to stabilize the cleavable complex formed with TOP1 and DNA. Two analogues with very potent TOP1-targeting activity, 3a and 4a, exhibited cytotoxic activity with IC50 values at or below 2 nM against RPMI8402. Compound 3a was active in vivo by either ip or po administration in the human tumor xenograft athymic nude mice model.

原文英語
頁(從 - 到)3333-3336
頁數4
期刊Bioorganic and Medicinal Chemistry Letters
12
發行號22
DOIs
出版狀態已發佈 - 十一月 18 2002
對外發佈Yes

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ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

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