• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>RSC Advances >Synthesis, biological evaluation and mechanism study of chalcone analogues as novel anti-cancer agents
【24h】

Synthesis, biological evaluation and mechanism study of chalcone analogues as novel anti-cancer agents

机译：Chalcone类似物作为新型抗癌剂的合成，生物学评价和机制研究

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 series of novel chalcone analogues were designed, synthesized and evaluated as anticancer agents. The results of antiproliferative activity tests showed that most of the analogues exhibited moderate to very good antiproliferative activities with GI(50) values in the micromol to sub-micromol range. Especially compound 10a gave 0.026 mu M to 0.035 mu M GI(50) for five cancer cell lines. The mechanistic studies including tubulin polymerization inhibition, disruption of microtubule dynamics and cell cycle arrest assay demonstrated that compound 10a could effectively inhibit in vitro cellular tubulin polymerization, interfere with the mitosis, resulting in a prolonged G2/M cell cycle arrest and ultimately lead to cell apoptosis of cancer cells. Taken together, these results suggested that 10a may became a promising lead compound for development of new anticancer drugs.
机译：设计了一系列新的Chalcone类似物，合成并评估为抗癌剂。 抗增殖活性试验的结果表明，大多数类似物表现出中等至非常好的抗增殖活性，MICROOL中的GI（50）值与亚微米范围。 特别是化合物10A对于五种癌细胞系，得到0.026μm至0.035μmgi（50）。 包括微管蛋白聚合抑制的机械研究，微管动力学和细胞周期延迟测定的破坏证明，化合物10a可以有效地抑制体外细胞纤维蛋白聚合，干扰有丝分裂，导致延长的G2 / m细胞周期停滞，最终导致细胞 癌细胞的凋亡。 总之，这些结果表明，10A可能成为新抗癌药物的有前途的铅化合物。

著录项

  • 来源
    《RSC Advances》 |2015年第83期|共8页
  • 作者

    Chen Jie; Yan Jun; Hu Jinhui; Pang Yanqing; Huang Ling; Li Xingshu;

  • 作者单位

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

    Sun Yat Sen Univ Sch Pharmaceut Sci Guangzhou 510006 Guangdong Peoples R China;

  • 收录信息
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 化学;
  • 关键词

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