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Acta Chimica Sinica ›› 2008, Vol. 66 ›› Issue (14): 1731-1734. Previous Articles     Next Articles

纺锤体驱动蛋白抑制剂的设计、合成与生物活性研究

阮秀琴a,b,c 尤启冬*,a,b 杨 蕾d 吴梧桐d   

  1. (a中国药科大学 江苏省肿瘤发生与干预重点实验室 南京 210009)
    (b中国药科大学 药物化学教研室 南京 210009)
    (c中国药科大学 物理化学教研室 南京 210009)
    (d中国药科大学 生命科学与技术学院 南京 210009)
  • 投稿日期:2007-12-10 修回日期:2008-01-22 发布日期:2008-07-28
  • 通讯作者: 尤启冬

Design, Synthesis and Biological Evaluation of Novel KSP Inhibitors

RUAN, Xiu-Qin a,b,c YOU, Qi-Dong *,a,b YANG, Lei d WU, Wu-Tong d   

  1. (a Key Laboratory of Carcinogenesis and Intervention of Jiangsu Province, China Pharmaceutical University,
    Nanjing 210009)
    (b Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009)
    (c Department of Physical Chemistry, China Pharmaceutical University, Nanjing 210009)
    (d School of Life and Technology, China Pharmaceutical University, Nanjing 210009)
  • Received:2007-12-10 Revised:2008-01-22 Published:2008-07-28
  • Contact: YOU, Qi-Dong

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The kinesin spindle protein (KSP/Eg5) is a potential target in cancer therapy.It, which has attracted great interest in discovery of compounds that inhibit KSP. Here, a series of 4-oxo-tetrahydro-β-carline derivatives 9a～94f have been designed and synthesized as a novel class of KSP inhibitor. The synthesized compounds were, and evaluated for their inhibition of aganist KSP. All compounds inhibited ATPase activity with IC50 below that of the analog Monastrol. 9c has an IC50＝0.065 μmol•L－1 for inhibition of KSP, ＞100-fold more active than Monastrol. The research results provide new candidate molecules for study of anticancer drugs.

Key words: kinesin spindle protein, 4-oxo-tetrahydro-β-carline, anticancer