...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis and biological evaluation of novel isoxazoles and triazoles linked 6-hydroxycoumarin as potent cytotoxic agents
【24h】

Synthesis and biological evaluation of novel isoxazoles and triazoles linked 6-hydroxycoumarin as potent cytotoxic agents

机译：新型异恶唑和三唑连接的6-羟基香豆素作为强效细胞毒剂的合成及生物学评价

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

A new series of diverse isoxazoles and triazoles linked 6-hydroxycoumarin (1) were synthesized using click chemistry approach. All the derivatives were subjected to 3-(4,5-dimethylthiazol-yl)-diphenyl tetrazoliumbromide (MTT) cytotoxicity screening against a panel of five different human cancer cell lines viz. prostate (PC-3), colon (HCT-116 and Colo-205), leukemia (HL-60) and lung (A-549) to check their cytotoxic potential. Interestingly, among the tested molecules, some of the analogs displayed better cytotoxic activity than the parent 6-hydroxycoumarin (1). Of the synthesized isoxazoles, compounds 10 and 13 showed the best activity with IC50 of 8.2 and 13.6 μM against PC-3 cancer cell line, while as, among the triazoles, compounds 23 and 25 were the most active with the IC50 of 10.2 and 12.6 μM against A-549 cancer cell line. The other derivatives showed almost comparable activity with that of the parent molecule. The present study resulted in identification of ortho substituted isoxazole and triazole derivatives of 6-hydroxycoumarin as effective cytotoxic agents against prostate (PC-3) and lung (A-549) cancer cell lines, respectively.
机译：使用点击化学方法合成了一系列新的各种异恶唑和三唑连接的6-羟基香豆素（1）。对所有衍生物对5-（4,5-二甲基噻唑基）-二苯基溴化四唑鎓（MTT）细胞毒性进行筛选，以检测一组五种不同的人类癌细胞系。前列腺（PC-3），结肠（HCT-116和Colo-205），白血病（HL-60）和肺（A-549）检查其细胞毒性潜力。有趣的是，在测试的分子中，某些类似物显示出比母体6-羟基香豆素更好的细胞毒活性（1）。在合成的异恶唑中，化合物10和13对PC-3癌细胞的活性最高，IC50为8.2和13.6μM，而在三唑中，化合物23和25的活性最高，IC50为10.2和12.6。针对A-549癌细胞系的μM。其他衍生物显示出与母体分子几乎可比的活性。本研究结果确定了6-羟基香豆素的邻位取代异恶唑和三唑衍生物分别作为针对前列腺癌（PC-3）和肺癌（A-549）癌细胞系的有效细胞毒剂。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号