1973-04-2Relevant articles and documents
SARs of a novel series of s-triazine compounds targeting vimentin to induce methuotic phenotype
Zhang, Lei,Qu, Zhipeng,Wu, Jianping,Yao, Shining,Zhang, Qingqing,Zhang, Tao,Mo, Lian,Yao, Qizheng,Xu, Ying,Chen, Ruihuan
, (2021/02/09)
Herein, we describe the design, synthesis and structure?activity relationships of a series of novel s-triazine compounds can induce methuotic phenotype in various types of cancer cells. (E)-1-(4-Chlorophenyl)-3-(4-((4-morpholino-6-styryl-1,3,5-triazine-2-yl)amino)phenyl)urea, compound V6, exhibited a striking methuotic phenotype with a minimal effective concentration of less than 10 nM in U87 glioblastoma cells. Based on structure?activity relationship studies, we designed and synthesized an active probe P1 that retained the full potential of V6 in inducing the methuotic phenotype in U87 glioblastoma cells. Using this probe following affinity-based proteomic profiling strategy, we identified vimentin as the specific target protein of compound V6. Molecular docking revealed that V6 can form hydrogen bonds with vimentin at 273R and 276Y in its rod domain.
Synthesis method of dihalogenated s-triazine
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Paragraph 0032-0035, (2021/04/14)
The invention discloses a synthesis method of dihalogenated s-triazine. The method comprises the following steps: dissolving a substituted nitrile compound and a halogenated nitrile compound in a certain solvent, adding a certain catalyst, and introducing halogenated hydrogen at a certain temperature for a certain period of time, and reacting to obtain the dihalogenated s-triazine. The invention provides a new reaction route for synthesizing the dihalogenated s-triazine, the dihalogenated s-triazine is prepared by taking the substituted nitrile compound and the halogenated nitrile compound as raw materials and adopting a one-step reaction, the reaction steps and process are saved, the process is simple and convenient, the cost is low, the product yield is high and reaches 99 percent or above, and moreover, a dangerous process of Grignard reaction is avoided in the synthesis process, the production risk is reduced, and meanwhile, the problem of environmental pollution is avoided.
NOVEL 2,4,6-TRISUBSTITUTED S-TRIAZINE COMPOUND, PREPARATION METHOD THEREFOR, AND USE THEREOF
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Paragraph 0069, (2019/04/05)
The present invention provides a 2,4,6-trisubstituted s-triazine compound represented by general formula (I) or pharmaceutically acceptable salts, prodrugs or solvates thereof, a preparation method therefor, and use of these compounds in preparing drugs for preventing or treating diseases associated with protein kinase and vimentin dysregulation, and cell vacuolization, and in particular, drugs for treating or preventing cancer growth and metastasis, tissue fibrosis and atherosclerosis.