Citation: Zhang Chenglu, Sun Xiaona, Pu Yuxin, Li Chuanyin, Sun Lijie, Wang Jing, Li Yizheng. Design, Synthesis and Activities of Multiheterocyclic Modified Novel Molecules Using 1, 3-Selenazole as Template[J]. Chinese Journal of Organic Chemistry, ;2017, 37(2): 440-454. doi: 10.6023/cjoc201607024 shu

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

  • Corresponding author: Zhang Chenglu, zhangchenglu@lnnu.edu.cn
  • Received Date: 15 July 2016
    Revised Date: 3 September 2016

    Fund Project: the Science and Technology Research Program of Liaoning Provincial Department of Education 2009A426

Figures(8)

  • 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.
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