应用化学2018，Vol.35Issue(2)：154-164,11.DOI:10.11944/j.issn.1000-0518.2018.02.170004
细胞分裂周期25磷酸酯酶B抑制剂双1,2,4-三唑多杂环分子的设计合成
Synthesis and Design of Multi-Heterocyclic Molecules with Duoble 1,2,4-Triazole Motifs as Inhibitors of Cell Division Cycle Protein 25 B Phosphatases
摘要
Abstract
Heterocyclic molecules containing 1,2,4-triazole motif are important for drug screening due to their better broad spectrum of bioactivities.For structure-activity relationship study, twenty-eight novel multi-heterocyclic molecules[TM1 ~TM3(a ~f)]and[TM4 ~TM5(a ~e)]containing duo 1,2,4-triazole motifs were synthesized by the conjugation with piperazine and s-triazine,respectively.The structures of target molecules were confirmed via infrared(IR),proton nuclear magnetic resonance(1H NMR)and high resolution mass spectrometry(HRMS).In order to investigate the effect of 4-amino substituent on 1,2,4-triazole for bioactivities, the comparison between compounds 6-morpholine-2,4-(5-thioether-4-amino-3-n-pentyl-1,2,4-triazole)-1,3,5-triazine(C),6-pyrrole-2,4-(5-mercapto-4-amino-3-n-pentyl-1,2,4-triazole)-1,3,5-triazine (D)and target molecules were also performed.The inhibitory activities against cell division cycle protein 25B (Cdc25B)phosphatases of synthesized molecules were evaluated.Twenty one molecules exhibit good activities,and nine among them are more potent than the positive control Na3VO4.关键词
1,2,4-三唑/哌嗪/三嗪/细胞分裂周期25磷酸酯酶B抑制剂Key words
1,2,4-triazole/piperazine/s-triazine/cell division cycle protein 25B inhibitor分类
化学化工引用本文复制引用
张成路,王静,李益政,李传银,孙晓娜..细胞分裂周期25磷酸酯酶B抑制剂双1,2,4-三唑多杂环分子的设计合成[J].应用化学,2018,35(2):154-164,11.基金项目
辽宁省教育厅科学技术项目资助(2009A426)Supported by the Technology Research Program of Liaoning Provincial Department of Education(No.2009A426) （2009A426）
