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

发布时间：2018-07-07 14:19

本文选题：-硒唑 + 多杂环　；参考：《有机化学》2017年02期

【摘要】：以取代1,3-硒唑为模板,分别利用1,2,4-三唑、四唑、VA二唑、吡唑、1,2,4-三嗪和丁二酰亚胺等修饰,首次设计合成了6类共22个目标分子,并利用IR,NMR和HRMS等波谱技术对目标分子进行了结构表征.评价了目标分子对Cdc25B的抑制活性,结果发现,13个目标分子具有较好的抑制活性,其中有5种目标分子的抑制活性高于阳性参照物Na_3VO_4有望成为抗肿瘤药物先导物.构效分析结果发现,在1,3-硒唑骨架上引入多氮杂环三唑、四唑和三嗪,引入含有氨基和巯基的噻二唑和VA二唑等有望获得活性优良的新型含硒有机分子.
[Abstract]:Six kinds of 22 target molecules were designed and synthesized by using substituted 1 ~ (3) -selenazole as template, using 1 ~ (2) C _ (2) -triazole, tetrazolium VA diazole, pyrazole 1 ~ (2 +) ~ (22) -triazine and succinimide, respectively, for the first time, a total of 22 target molecules of 6 classes were designed and synthesized. The structure of the target molecule was characterized by IR NMR and HRMS. The inhibitory activity of the target molecule against Cdc25B was evaluated. The results showed that 13 target molecules had better inhibitory activity, and 5 of them had higher inhibitory activity than the positive reference Na3VOS4, which was expected to be the leader of antitumor drugs. The results of structure-activity analysis showed that polyazacyclic triazole, tetrazole and triazine, thiadiazoles containing amino groups and thiadiazole and VA diazole could be added to the skeleton of 1-azo-3-selenazole to obtain novel selenium-containing organic molecules with good activity.
【作者单位】：辽宁师范大学化学化工学院;
【基金】：辽宁省教育厅科学技术研究(No.2009A426)资助项目~~
【分类号】：O627.61;TQ460.1

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