Ring fusion strategy for the synthesis of anthra[2,3-d ]oxazole-2-thione-5,10-dione homologues as DNA topoisomerase inhibitors and as antitumor agents

Chun Liang Chen, Fei Lan Liu, Chia Chung Lee, Tsung Chih Chen, Wen Wei Chang, Jih Hwa Guh, Ahmed Atef Ahmed Ali, Deh Ming Chang, Hsu Shan Huang

研究成果: 雜誌貢獻文章同行評審

16 引文 斯高帕斯(Scopus)

摘要

The efficient synthesis of mono-substituted anthraquinones and ring fusion into anthra[2,3-d]oxazole-2-thione-5,10-dione derivatives were developed, and all the compounds were tested for their cytotoxicity against PC-3 cancer cell lines. Compounds 8, 14, 17 and 23 were selected by the NCI and 12, 17 and 19 were evaluated for topoisomerase I-mediated DNA relaxation. Among them, 17 appeared to be the most active compound of this series and not only showed higher inhibition when indicated from the low IC50values against PC-3 cancer cell line but also attenuated the in vitro topoisomerase I-mediated DNA relaxation at low micromolar concentrations. All test compounds exhibited different cytostatic and cytotoxic activities for further developing potential anticancer drugs.
原文英語
頁(從 - 到)30-38
頁數9
期刊European Journal of Medicinal Chemistry
87
DOIs
出版狀態已發佈 - 十一月 24 2014

ASJC Scopus subject areas

  • 藥物發現
  • 有機化學
  • 藥理
  • 醫藥 (全部)

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