Determination cytotoxicity of [1,2,4]triazolo[4,3-a]-pyrazine derivatives

• Main Authors: Кристина Юріївна Куликовська, Ірина Олександрівна Журавель
• Format: Article
• Language: English
• Published: PC Technology Center 2015-11-01
• Series: ScienceRise
• Subjects: [1; 2; 4]triazolo[4; 3-а]pyrazines; cytotoxicity; cytotoxic concentration; test system CellTiter-Glo; cell culture; tubertsydyn; taxol
• Online Access: http://journals.uran.ua/sciencerise/article/view/54989

<p>With test systems CellTiter-Glo was determined the cytotoxicity of series N⁷-aryl/benzyl-3-tioxo-2,3-dihydro-7Н-[1,2,4]triazolo-[4,3-а]pyrazin-8-ones, their 3-S- acetamides and 3-S-benzyl derivatives. The synthesis of the compounds performed based on the previously developed and published scheme. Structure and purity of the compounds proved with ¹H-NMR and element analysis.</p><p><strong>Methods</strong><strong>.</strong> The method is based on determining the number of viable cells in culture by intensity of luminescence mixture of cell suspension of prostate cancer Du₁₄₅, solution of the substance and CellTiter-Glo reagent. Tubercidin and taxol were used as reference drugs. The parameter СK₅₀, that has been set according to a study, describes the ability of analyzed substances induce cell death.<strong></strong></p><p><strong>Results</strong><strong>.</strong> Cytotoxic concentration of synthesized 3-substituted N⁷-aryl/benzyl-2,3-dihydro-7Н-[1,2,4]triazolo-[4,3-а]pyrazine-8-ones not exceed the maximum concentration of compounds, which were tested, and was above 30 mkM. This demonstrates the complete absence of negative impact of these substances on cells of prostate cancer Du₁₄₅.</p><p><strong>Conclusions</strong><strong>. </strong>Found that these compounds do not exhibit toxic effects on living cells, making the actual possibility of developing new effective and safe drugs on their base. Also inappropriate to search anticancer drugs among of the N⁷-aryl/benzyl-2,3-dihydro-7Н-[1,2,4]triazolo-[4,3-а]pyrazine-8-one derivatives</p>