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 |
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頁(從 - 到) | 30-38 |
頁數 | 9 |
期刊 | European Journal of Medicinal Chemistry |
卷 | 87 |
DOIs | |
出版狀態 | 已發佈 - 11月 24 2014 |
ASJC Scopus subject areas
- 藥物發現
- 有機化學
- 藥理
- 醫藥 (全部)