Citation: ZHANG Chenglu, XI Huan, SHA Yuting, SUN Xiaona, LI Chuanyin, WANG Jing, LI Yizheng. Synthesis and Bioactivity of Novel Bis-heterocyclic Amide Modified Sulfide Derivatives[J]. Chinese Journal of Applied Chemistry, ;2017, 34(3): 308-315. doi: 10.11944/j.issn.1000-0518.2017.03.160352 shu

Synthesis and Bioactivity of Novel Bis-heterocyclic Amide Modified Sulfide Derivatives

College of Chemistry and Chemical Engineering, Liaoning Normal University, Dalian, Liaoning 116029, China

Corresponding author: ZHANG Chenglu, zhangchenglu@lnnu.edu.cn
Received Date: 2 September 2016
Revised Date: 20 October 2016
Accepted Date: 28 November 2016

Fund Project: Supported by Technology Research Program of Liaoning Provincial Department of Education No.2009A426

Figures(2)

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(PTP1B) 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±0.22) 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.
- triazole,
- thiadiazole,
- protein tyrosine phosphatase 1B,
- cell division cycle 25B,
- inhibitors
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