Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (2): 440-454.DOI: 10.6023/cjoc201607024 Previous Articles     Next Articles



张成路, 孙晓娜, 蒲雨昕, 李传银, 孙丽杰, 王静, 李益政   

  1. 辽宁师范大学化学化工学院 大连 116029
  • 收稿日期:2016-07-15 修回日期:2016-09-03 发布日期:2016-10-09
  • 通讯作者: 张成路
  • 基金资助:


Design, Synthesis and Activities of Multiheterocyclic Modified Novel Molecules Using 1,3-Selenazole as Template

Zhang Chenglu, Sun Xiaona, Pu Yuxin, Li Chuanyin, Sun Lijie, Wang Jing, Li Yizheng   

  1. College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian 116029
  • Received:2016-07-15 Revised:2016-09-03 Published:2016-10-09
  • Supported by:

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

Six kinds, twenty-two novel target molecules were first designed and synthesized by using substituted 1,3-selenazole as a template, which were modified by 1,2,4-triazole, tetrazole, oxadiazole, pyrazole, 1,2,4-triazine and succinic imide respectively. Their structures were confirmed by IR, NMR and HRMS. The inhibitory activities of the target molecules against cell division cycle 25B phosphatase (Cdc25B) were evaluated. As a result, thirteen compounds exhibited good inhibitory activities. The IC50 values of five compounds were lower than the positive reference Na3VO4 and were expected to be anticancer drugs leading compounds. The analysis of structure-activity relationship found that the introduction of multinitrgon-heterocyclic triazole, tetrazole and triazine, thiadiazole and oxadiazole containing amino or mercapto group onto 1,3-selenazole were expected to obtain novel excellent bioactivity organic selenium containing molecules.

Key words: 1,3-selenazole, multi-heterocycle, Cdc25B inhibitor