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Synthesis of Novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene Derivatives and Their Biological Evaluation Against Protein Tyrosine Phosphatase 1B.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2015 May 21 , DOI: 10.1111/cbdd.12587
Wen-Long Wang 1, 2 , Xia Chen 1 , Li-Xin Gao 2 , Li Sheng 2 , Jing-Ya Li 2 , Jia Li 2 , Bainian Feng 1
Affiliation  

A series of novel 3-aryl-1-oxa-2,8-diazaspiro[4.5]dec-2-ene derivatives were designed, synthesized, and evaluated as a new class of inhibitors against protein tyrosine phosphatase 1B. Among them, compound 6f displayed moderate inhibitory activity with IC50 of 2.87 +/- 0.24 mum and can be used as a novel lead compound for the design of inhibitors of protein tyrosine phosphatase 1B.

中文翻译:

新型3-芳基-1-氧杂-2,8-二氮杂螺[4.5]癸-2-烯衍生物的合成及其对蛋白质酪氨酸磷酸酶1B的生物学评价。

设计,合成和评估了一系列新颖的3-芳基-1-氧杂-2,8-二氮杂螺[4.5]癸-2-烯衍生物,作为针对蛋白质酪氨酸磷酸酶1B的新型抑制剂。其中,化合物6f表现出中等的抑制活性,IC50为2.87 +/- 0.24微米,可用作设计蛋白质酪氨酸磷酸酶1B抑制剂的新型先导化合物。
更新日期:2017-01-31
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