首页 / 院系成果 / 成果详情页

Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin  期刊论文  

  • 编号:
    413e5f0d-13b8-4ccb-9e0b-a9949cb1da8f
  • 作者:
    Zhou, Pengfei[1];Liu, Yan[2];Zhou, Lu(周璐)[1]Zhu, Kongkai[2];Feng, Kechang[1];Zhang, Hao[2];Liang, Yuru[1];Jiang, Hualiang[2];Luo, Cheng[2];Liu, Mingming(刘明明)*[1]Wang, Yang(王洋)*[1]
  • 语种:
    English
  • 期刊:
    JOURNAL OF MEDICINAL CHEMISTRY ISSN:0022-2623 2016 年 59 卷 22 期 (10329 - 10334) ; NOV 24
  • 收录:
  • 摘要:

    A series of chiral,beta-lactam bridged analogues (3-substituted 1,4-diaryl-2-azetidinones) of combretastatin A-4 (CA-4) were synthesized asymmetrically, and their antitumor activities were evaluated in vitro and in vivo. The cocrystal structure of tubulin in complex with compound 9 was determined by X-ray crystallography, which showed that 9 binds to the same site as colchicine with similar binding mode, and the absolute configuration of its C-4 was first identified and demonstrated to be critically important for their antiproliferative activities.

  • 推荐引用方式
    GB/T 7714:
    Zhou Pengfei,Liu Yan,Zhou Lu, et al. Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin [J].JOURNAL OF MEDICINAL CHEMISTRY,2016,59(22):10329-10334.
  • APA:
    Zhou Pengfei,Liu Yan,Zhou Lu,Zhu Kongkai,&Wang Yang.(2016).Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin .JOURNAL OF MEDICINAL CHEMISTRY,59(22):10329-10334.
  • MLA:
    Zhou Pengfei, et al. "Potent Antitumor Activities and Structure Basis of the Chiral beta-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin" .JOURNAL OF MEDICINAL CHEMISTRY 59,22(2016):10329-10334.
浏览次数:3 下载次数:0
浏览次数:3
下载次数:0
打印次数:0
浏览器支持: Google Chrome   火狐   360浏览器极速模式(8.0+极速模式) 
返回顶部