437608-70-3Relevant academic research and scientific papers
Discovery of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as novel, potent and selective c-Met kinase inhibitors: Synthesis, SAR study, and biological activity
Zhang, Li,Zhao, Jingyun,Zhang, Beichen,Lu, Tao,Chen, Yadong
, p. 809 - 816 (2018)
A series of [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives were designed, synthesized and evaluated for their biological activity. Most of these compounds showed potent activities against c-Met kinase and cell growth inhibition. The most promising compound, 7d, has the IC50 values of 2.02 and 88 nM to inhibit c-Met kinase activity and cell growth in the MKN45 cell line, respectively. In addition, 7d is highly selective to c-Met and exhibits over 2500-fold selective inhibition to 16 tyrosine kinases evaluated.
Discovery, optimization and biological evaluation for novel c-Met kinase inhibitors
Yuan, Haoliang,Liu, Qiufeng,Zhang, Li,Hu, Shihe,Chen, Tiantian,Li, Huifang,Chen, Yadong,Xu, Yechun,Lu, Tao
, p. 491 - 502 (2018)
The c-Met kinase has emerged as an attractive target for developing antitumor agents because of its close relationship with the development of many human cancers, poor clinical outcomes and even drug resistance. A series of novel c-Met kinase inhibitors h
Preparation method and applications of triazolo-thiadiazole c-Met kinase inhibitor
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Paragraph 00850087, (2019/07/04)
The invention relates to the field of pharmaceutical chemistry, and specifically relates to [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives, a preparation method thereof, a pharmaceutical composition comprising the same, and medical applications thereof, in particular, an application as a c-Met kinase inhibitor.
INHIBITORS OF C-MET AND USES THEREOF
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Page/Page column 79-80; Figure 3; Figure 9, (2008/06/13)
The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment o
Synthesis, antibacterial and antifungal activity of 4-substituted-5-aryl-1, 2,4-triazoles
Colanceska-Ragenovic, Katica,Dimova, Vesna,Kakurinov, Vlado,Molnar, Dora Gabor,Buzarovska, Aleksandra
, p. 815 - 824 (2007/10/03)
A few 4-allyl/amino-5-aryl-1,2,4-triazoles were synthesized and tested for antibacterial and antifungal effects against Escherichia coli, Bacillus subtilis, Salmonella enteritidis, Staphylococcus aureus, Aspergillus niger and Candida albicans. 4-Allyl-5-aryl-1,2,4-triazoles were obtained by the oxidative cyclization of the appropriate 1-substituted-4-allylthiosemicarbazides and 4-amino-5-aryl-1,2,4-triazoles were obtained by cyclization of the potassium salts of appropriately substituted dithiocarbazinic acids with hydrazine hydrate. The new synthesized compounds were characterized using IR, 1H- NMR, 13C-NMR and UV spectral data together with elemental analysis.
