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Progress in Chemistry 2010, Vol. 22 Issue (01): 153-162 Previous Articles   Next Articles

• Invited Article •

Kinesin Spindle Protein Inhibitors

Jiang Cheng1,2;  Zhang Xiaojin1,2;  Shen Zheng1,2;  You Qidong1,2**   

  1. (1. Jiangsu Key Laboratory of Carcinogenesis and Intervention, 2. Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China)
  • Received: Revised: Online: Published:
  • Contact: You Qidong E-mail:youqidong@gmail.com
  • Supported by:

    National Natural Science Foundation of China

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Inhibition of kinesin spindle protein(KSP) represents a novel and specific mechanism to target the mitotic spindle that may be devoid of the neuropathy-associated side effects common to the agents that target microtubules. Since the discovery of monastrol, the first selective small molecular inhibitor of KSP, many types of KSP inhibitors have been reported. In this review we describe the development of different types of KSP inhibitors. The structures and functions of KSP and the use of which as a novel target in the research of anticancer agents are introduced. The structure-activity relationship of some KSP inhibitors and the perspective of the study on KSP inhibitors are also discussed.

Contents
1 Introduction
2 Structure and functions of KSP
3 KSP Inhibitors
3.1 Adociasulfate 2
3.2 Monastrol and its analogues
3.3 Pyrimidinone or pyrimidinone-like compounds
3.4 Dihydropyrazoles, dihydropyrroles and their analogues
3.5 Tetrahydro-β-carbolines
3.6 Bi-aryls as ATP-competitive inhibitors of KSP
3.7 Other KSP inhibitors
4 Conclusion

Key words: KSP, anti-cancer, inhibitors, Eg5

CLC Number: 

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Abstract

Kinesin Spindle Protein Inhibitors