anticancer activity

The article by authors Shupeniuk V.I., Taras T.M., Sabadakh O.P., Bolibruch L.D., Zhurakhivska L.R. “Triazenes on the basis of 4-imidazole substituted antraquinone as the potential inhibitors of proteins” devoted to the study of the structure of triazenes on the basis of 4-imidazole substituted 9,10-anthraquinone, depending on the calculation of their probable effect on proteins using the DIGEP-Pred program.

The synthesis and antitumor activity screening of 1,2,4-triazino[5,6-b]indoles based conjugates were performed. Reaction between 3-mercapto-1,2,4-triazino[5,6-b]indoles and several N-arylchloroacetamides yielded 3S-substituted 1,2,4-triazino[5,6-b]indoles. Based on 3-hydrazine-1,2,4-triazino[5,6-b]indoles the new 4-thiazolidinones have been synthesized. Seven synthesized compounds were tested for their anticancer activity in NCI60 cell lines.

Following the N-alkylation reaction of starting 2-chloro-N-(5-aryl-1,3,4-oxadiazol-2-yl)-acetamides 1a-c with 2,4-thiazolidinedione or 5-sudstituted isatins the corresponding non-condensed oxadiazole derivatives with thiazolidine 2a-c or isatin 4a-h fragments were synthesized. The obtained compounds have been used in Knoevenagel condensation with 5R-isatin (for 2a-c) or 4-thiazolidinone derivatives (for 4a-h) for synthesis of the appropriate 5-ylidenederivatives 3a-g, 5a-k and 6a-d.