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


  • Кристина Юріївна Куликовська National University of Pharmacy 53 Pushkinska str., Kharkiv, Ukraine, 61002, Ukraine
  • Ірина Олександрівна Журавель National University of Pharmacy 53 Pushkinska str., Kharkiv, Ukraine, 61002, Ukraine



[1, 2, 4]triazolo[4, 3-а]pyrazines, cytotoxicity, cytotoxic concentration, test system CellTiter-Glo, cell culture, tubertsydyn, taxol


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.

Methods. 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.

Results. 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.

Conclusions. 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

Author Biographies

Кристина Юріївна Куликовська, National University of Pharmacy 53 Pushkinska str., Kharkiv, Ukraine, 61002

Candidate of Pharmaceutical Sciences, assistant

Department of Toxicological Chemistry

Ірина Олександрівна Журавель, National University of Pharmacy 53 Pushkinska str., Kharkiv, Ukraine, 61002

Doctor of chemical sciences, professor

Department of Toxicological Chemistry


Order of the Ministry of Health of Ukraine №944 of 14.12.2009 «On approval of the pre-clinical study of medicinal products and expert evaluation of pre-clinical study of medicinal products». Available at:

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Pharmaceutical Sciences