Sun, Lingyi; Bera, Hriday; Chui, Wai Keung published an article in European Journal of Medicinal Chemistry. The title of the article was 《Synthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase》.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine The author mentioned the following in the article:
Thymidine phosphorylase (TP) is an enzyme that promotes tumor growth and metastasis and therefore is an attractive druggable target. Using a reported TP inhibitor, 7-deazaxanthine (7DX), as the lead compound; this study was set up to evaluate whether pyrazolo[1,5-a][1,3,5]triazin-2,4-diones and pyrazolo[1,5-a][1,3,5]triazin-2-thioxo-4-ones would exhibit TP inhibitory activity. The pyrazolo[1,5-a][1,3,5]triazine nucleus was constructed using a reaction that annulated the 1,3,5-triazine ring onto a pyrazole scaffold. Among the 52 compounds synthesized and tested, it was found that 1,3-dihydro-pyrazolo[1,5-a][1,3,5]triazin-2-thioxo-4-ones exhibited various extent of inhibitory activity against TP. The best compound I, which bears a para-substituted pentafluorosulfur group, showed an IC50 value of 0.04 μM, which was around 800 times more potent than the 7DX (IC50 = 32 μM) under the same bioassay conditions. The results of the study suggested that a substituent with +σ and +π properties inserted at position 4 of a Ph ring that is attached to position 8 of the pyrazolo[1,5-a][1,3,5]triazin-2-thioxo-4-one scaffold would give excellent TP inhibitory action. In addition, I was found to be a non-competitive inhibitor thus suggested that it might interact with TP at a position different from the substrate binding site. In the experimental materials used by the author, we found 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine(cas: 1015845-73-4Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine)
4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine(cas: 1015845-73-4) belongs to anime. Amines characteristically form salts with acids; a hydrogen ion, H+, adds to the nitrogen. With the strong mineral acids (e.g., H2SO4, HNO3, and HCl), the reaction is vigorous. Salt formation is instantly reversed by strong bases such as NaOH. Neutral electrophiles (compounds attracted to regions of negative charge) also react with amines; alkyl halides (R′X) and analogous alkylating agents are important examples of electrophilic reagents.Recommanded Product: 4-(4-(tert-Butyl)phenyl)-1H-pyrazol-3-amine
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics