33263-03-5Relevant articles and documents
Triazole-Based Inhibitors of the Wnt/β-Catenin Signaling Pathway Improve Glucose and Lipid Metabolisms in Diet-Induced Obese Mice
Obianom, Obinna N.,Ai, Yong,Li, Yingjun,Yang, Wei,Guo, Dong,Yang, Hong,Sakamuru, Srilatha,Xia, Menghang,Xue, Fengtian,Shu, Yan
, p. 727 - 741 (2019/01/21)
Wnt/β-catenin signaling pathway is implicated in the etiology and progression of metabolic disorders. Although lines of genetic evidence suggest that blockage of this pathway yields favorable outcomes in treating such ailments, few inhibitors have been used to validate the promising genetic findings. Here, we synthesized and characterized a novel class of triazole-based Wnt/β-catenin signaling inhibitors and assessed their effects on energy metabolism. One of the top inhibitors, compound 3a, promoted Axin stabilization, which led to the proteasome degradation of β-catenin and subsequent inhibition of the Wnt/β-catenin signaling in cells. Treatment of hepatocytes and high fat diet-fed mice with compound 3a resulted in significantly decreased hepatic lipid accumulation. Moreover, compound 3a improved glucose tolerance of high fat diet-fed mice without noticeable toxicity, while downregulating the genes involved in the glucose and fatty acid anabolisms. The new inhibitors are expected to be further developed for the treatment of metabolic disorders.
Copper-catalyzed consecutive reaction to construct quinazolin-4(3H)-ones and pyrido[2,3-d]pyrimidin-4(3H)-ones
Li, Ting,Chen, Minglu,Yang, Lei,Xiong, Zhengxin,Wang, Yongwei,Li, Fei,Chen, Dongyin
, p. 868 - 874 (2016/01/20)
An efficient and practical copper-catalyzed consecutive synthesis of quinazolin-4(3H)-ones and pyrido[2,3-d]pyrimidin-4(3H)-ones from easily available 2-halobenzamides (or 2-halonicotinamides), aldehydes, and sodium azide has been developed, which gave the corresponding target products in 50-95% yields for 29 examples. This remarkable consecutive process involved sequential copper-catalyzed SNAr, reduction, cyclization, and oxidation. Notably, this work would provide a novel synthetic strategy for bioactive molecules containing quinazolinone class skeletons.
Template synthesis of benzannulated N-heterocyclic carbene ligands
Hahn, F. Ekkehardt,Langenhahn, Volker,Meier, Nicole,Luegger, Thomas,Fehlhammer, Wolf Peter
, p. 704 - 712 (2007/10/03)
The reaction of 2-azidophenyl isocyanide (7) with [M(CO)5(thf)] (M = Cr, W) yields the isocyanide complexes [M(CO)5(7)] (M = Cr 8, M = W 9). Complexes 8 and 9 react with tertiary phosphines such as triphenylphosphane at the azido fun
