Synthesis and Evaluation of Terbenzimidazoles as Topoisomerase I Inhibitors

Qun Sun, Barbara Gatto, Chiang Yu, Angela Liu, Leroy F. Liu, Edmond J. LaVoie

研究成果: 雜誌貢獻文章同行評審

79 引文 斯高帕斯(Scopus)

摘要

The synthesis and pharmacological activity of a series of terbenzimidazoles are described. The ability of these derivatives to induce DNA cleavage in the presence of topoisomerase I was evaluated in vitro. These analogs were also assayed for their cytotoxicity in RPMI 8402 cells and the camptothecin-resistant CPT-K5 cells. In addition the potential for these compounds to serve as substrates for MDR1 was also determined. Several terbenzimidazoles exhibited similar cytotoxicity against variants of human tumor cells that either overexpress MDR1 or are camptothecin-resistant.

原文英語
頁(從 - 到)3638-3644
頁數7
期刊Journal of Medicinal Chemistry
38
發行號18
DOIs
出版狀態已發佈 - 九月 1 1995

ASJC Scopus subject areas

  • 分子醫學
  • 藥物發現

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