应用化学2017，Vol.34Issue(3)：308-315,8.DOI:10.11944/j.issn.1000-0518.2017.03.160352
新型双杂环修饰的酰胺硫醚衍生物的合成和生物活性
Synthesis and Bioactivity of Novel Bis-heterocyclic Amide Modified Sulfide Derivatives
摘要
Abstract
Sixteen novel double-heterocyclic modified amide sulfide derivatives containing 1,2,4-triazole and 1,3,4-thiadiazole were designed and synthesized,and their structures were characterized.The inhibitory activities of synthesized molecules against cell division cycle 25B(Cdc25B) of protein tyrosine phosphatase 1B (PTP1 B) were evaluated.The results show that all target molecules exhibit good inhibitory activity against PTP1B.Compounds 8-C-d and 8-D-c have the optimal inhibition.Their half maximal inhibitory concentration (IC50) values are (1.19 ± O.22) mg/L and (1.08 ± 0.09) mg/L,respectively,which are lower than that of positive reference oleanolic acid(IC50 =(1.27 ±0.19) mg/L).They are expected to be anti-diabetic drug leading compounds.The target molecules also exhibit good inhibitory activities against Cdc25B.The IC50 values of compounds 8-A-d,8-C-d and 8-D-c are higher than that of positive reference Na3VO4 (IC50 =(1.25 ±0.14) mg/L),which are expected to be anticancer drug leading compounds.关键词
三唑/噻二唑/蛋白酪氨酸磷酸酶1B/细胞分裂周期25磷酸酶B/抑制剂Key words
triazole/thiadiazole/protein tyrosine phosphatase 1B/cell division cycle 25B/inhibitors分类
化学化工引用本文复制引用
张成路,袭焕,沙禹廷,孙晓娜,李传银,王静,李益政..新型双杂环修饰的酰胺硫醚衍生物的合成和生物活性[J].应用化学,2017,34(3):308-315,8.基金项目
辽宁省教育厅科学技术项目资助(2009A426)Supported by Technology Research Program of Liaoning Provincial Department of Education (No.2009A426) （2009A426）
