Chinese Journal of Organic Chemistry >
Synthesis and Bioactivity Evaluation of Novel 1, 3, 5-Triazine-1H-pyrazole-triazol-ethiadiazole Derivatives
Received date: 2017-04-17
Revised date: 2017-06-28
Online published: 2018-01-03
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
Zhang Chenglu , Li Chuanyin , Gu Yaodong , Sun Xiaona , Tang Jie , Wang Jing , Li Yizheng , Wang Huayu . Synthesis and Bioactivity Evaluation of Novel 1, 3, 5-Triazine-1H-pyrazole-triazol-ethiadiazole Derivatives[J]. Chinese Journal of Organic Chemistry, 2018 , 38(5) : 1223 -1232 . DOI: 10.6023/cjoc201704028
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