Chin. J. Org. Chem. ›› 2018, Vol. 38 ›› Issue (5): 1223-1232.DOI: 10.6023/cjoc201704028 Previous Articles     Next Articles



张成路, 李传银, 顾耀东, 孙晓娜, 唐杰, 王静, 李益政, 王华玉   

  1. 辽宁师范大学化学化工学院 大连 116029
  • 收稿日期:2017-04-17 修回日期:2017-06-28 发布日期:2018-01-03
  • 通讯作者: 张成路,
  • 基金资助:


Synthesis and Bioactivity Evaluation of Novel 1, 3, 5-Triazine-1H-pyrazole-triazol-ethiadiazole Derivatives

Zhang Chenglu, Li Chuanyin, Gu Yaodong, Sun Xiaona, Tang Jie, Wang Jing, Li Yizheng, Wang Huayu   

  1. College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029
  • Received:2017-04-17 Revised:2017-06-28 Published:2018-01-03
  • Contact: 10.6023/cjoc201704028
  • Supported by:

    Project supported by the Science and Technology Research Program of Liaoning Provincial Department of Education (No. 2009A426).

Twenty-one novel 1, 3, 5-triazine-1H-pyrazole-triazolethiadiazole derivatives are designed and synthesized, in which the excellent pharmacological activitive pyrazole is used as key skeleton by connecting 1, 3, 5-triazine and introducing triazolothiadiazole. The structures of 21 target compounds are characterized by IR, 1H NMR and HRMS. The inhibitory activities of 21 novel target products against Cdc25B and PTP1B are evaluated. As a result, most of the target compounds exhibit excellent inhibitory activities. In the Cdc25B inhibitory activity test, 14 target compounds have higher inhibitory activities than the positive reference sodium orthovanadate, and they are expected to be potential of Cdc25B inhibitors. In the PTP1B inhibitory activity test, 9 target compounds have better inhibitory activities than the control oleanolic acid, and they are expected to be potential of PTP1B inhibitors.

Key words: pyrazole, 1, 3, 5-triazine, triazolothiadiazole, Cdc25B inhibitor, PTP1B inhibitor