A series of novel 3-azolylpyrazolo[5,1-c][1,2,4]triazines was synthesized by reaction of 3-substituted pyrazole-5-diazonium salts with β-azolyl enamines in an efficient fashion. The structures of the compounds prepared were characterized by NMR spectroscopy, massspectrometry, elemental and X-ray diffraction analyses. Plausible mechanisms were formulated.

The detailed study of an interaction of β-1,2,3-thiadiazolyl enamines with azoles containing diazo function allowed to establish the difference in the reactivity of azole-5-diazonium salts and 5-diazoazoles, which leads to...

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The work presents the results of study the cytotoxic activity of new azoloazine derivatives to establish the potential its possibility of use as antitumor agents, including for chemotherapy of metastatic breast cancer. The relevance of the work is due to the wide spread of oncological diseases and high cancer mortality, which dictates the need to constantly obtain cell lines and improve cultivation protocols for testing new antitumor drugs and obtaining new information about the chemistry of cancer. The culturing MCF-7 cells and determining cytotoxicity in a methyltetrazolium test are base methods used in this study. Comparative cytotoxicity was carried out by determining the concentration causing 50 % cell death for 11 azolotriazine derivatives taken at concentrations from 0.25 to 10.0 µM/L. Epirubicin, widely used in breast cancer chemotherapy, we used as a comparison drug. As a result, it was found that not all substances have toxic properties, despite the similar chemical structure and mechanism of action on the cell. The least toxic substances 10 and 11, in which, at the maximum studied concentration of 10 µM/L, cell survival was 86 and 75 %, respectively. The most toxic compounds against MCF-7 cells are substances 4 and 9 derivatives of with cytotoxicity indicators higher, respectively, by 11.0 and 3.1 highly compared to Epirubicin. The obtained data can be used as a basis for the selection of substances 4 and 9 for further study of their properties on cell models and laboratory animals as substances with potential anticancer activity/