103989-34-0Relevant articles and documents
1H and 13C NMR - Spectroscopy of substituted 1,2,3-triazoles
Sun, Xiao-Wen,Xu, Peng-Fei,Zhang, Zi-Yi
, p. 459 - 460 (1998)
1-Aryl-4-carboxy-5-methyl-1,2,3-triazoles were prepared by the condensation of aryl azides with ethyl acetoacetate. The structures of these compounds were characterized by MS, IR and 1H and 13C NMR spectroscopy. The measured and calc
Discovery and biological evaluation of novel 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety as c-Met kinase inhibitors
Zhou, Shunguang,Liao, Huimin,Liu, Mingmei,Feng, Guobing,Fu, Baolin,Li, Ruijuan,Cheng, Maosheng,Zhao, Yanfang,Gong, Ping
, p. 6438 - 6452 (2014)
A series of 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives possessing 1,2,3-triazole-4-carboxamide moiety were designed, synthesized and evaluated for their in vitro biological activities against c-Met kinase and five typical cancer cell lines (A549, H460, HT-29, MKN-45 and U87MG). Most compounds showed moderate to excellent antiproliferative activity. In this study, a promising compound 34, with a c-Met IC50 value of 1.04 nM, was identified as a multitargeted receptor tyrosine kinase inhibitor. The SAR analyses indicated that compounds with halogen group, especially fluoro group, at 4-position on the phenyl ring (moiety B) have potent antitumor activity, and methylation on the 5-atom linker played an important role in the c-Met enzymatic activity.
Design, synthesis and biological studies of some new imidazole-1,2,3-triazole hybrid derivatives
Dong, Hong-Ru,Huo, Guo-Yong,Wu, Jian-Guo
, (2022/02/14)
Some new 4-((1H-imidazol-1-yl)diarylmethyl)-5-methyl-1-aryl-1H-1,2,3-triazoles 7a-i were designed and synthesized by the one-pot reaction of diaryl-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)methanol compounds with 1H-imidazole. The new compounds 7a-i were ch
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.
WNT SIGNALING PATHWAY INHIBITORS FOR TREATMENTS OF DISEASE
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Paragraph 00167; 00183; 00184, (2017/09/15)
Compounds and compositions are provided as inhibitors of the Wnt/β-catenin pathway for the treatment of diseases that implicate the same.
Synthesis of 1,2,4- and 1,3,4-oxadiazoles from 1-aryl-5-methyl-1H-1,2,3- triazole-4-carbonyl chlorides
Obushak,Pokhodylo,Pidlypnyi,Matiichuk
scheme or table, p. 1522 - 1527 (2009/06/28)
5-Substituted 2-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)-1,3,4-oxadiazoles were synthesized by reaction of 1-aryl-5-methyl-1H-1,2,3-triazole-4-carbonyl chlorides with the corresponding 5-substituted 1H-tetrazoles. 5-Methyl-1-phenyl-1H-1,2,3-triazole-4-carb
