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Journal of Chinese Pharmaceutical Sciences ›› 2016, Vol. 25 ›› Issue (10): 726-736.DOI: 10.5246/jcps.2016.10.081

• Original articles • Previous Articles     Next Articles

Design, synthesis and evaluation of novel non-ATP competitive CHK1 inhibitors as chemotherapy sensitizing agents

Yuanxin Li, Zifei Han, Chao Tian*, Zhili Zhang*, Junyi Liu   

  1. Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China
  • Received:2016-05-15 Revised:2016-06-20 Online:2016-10-27 Published:2016-07-10
  • Contact: Tel.: +86-010-82805203, E-mail: tianchao@bjmu.edu.cn
  • Supported by:

    National Natural Science Foundation of China (Grant No. 21302007).

Abstract:

A series of urea-based compounds containing purine moieties were designed and synthesized as novel non-ATP competitive CHK1 inhibitors. The biological evaluation showed that several target compounds exhibited more potent inhibitory effects against CHK1 than the lead compound. In addition, one particular compound displayed synergistic effects with gemcitabine against HT29 cells.

Key words: CHK1 inhibitors, Non-ATP competitive, Anti-cancer synergistic effect

CLC Number: 

Supporting: