1,3-硒唑为模板多种杂环修饰的新型分子的设计、合成及活性研究
收稿日期: 2016-07-15
修回日期: 2016-09-03
网络出版日期: 2016-10-09
基金资助
辽宁省教育厅科学技术研究(No.2009A426)资助项目.
Design, Synthesis and Activities of Multiheterocyclic Modified Novel Molecules Using 1,3-Selenazole as Template
Received date: 2016-07-15
Revised date: 2016-09-03
Online published: 2016-10-09
Supported by
Project supported by the Science and Technology Research Program of Liaoning Provincial Department of Education (No. 2009A426).
张成路 , 孙晓娜 , 蒲雨昕 , 李传银 , 孙丽杰 , 王静 , 李益政 . 1,3-硒唑为模板多种杂环修饰的新型分子的设计、合成及活性研究[J]. 有机化学, 2017 , 37(2) : 440 -454 . DOI: 10.6023/cjoc201607024
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
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