Synthesis, cytotoxicity and effects of some 1,2,4-triazole and 1,3,4-thiadiazole derivatives on immunocompetent cells

Novel derivatives of 4,5-substituted-1,2,4-triazole-thiones and 2,5-substituted-1,3,4-thiadiazoles were synthesized and evaluated for their cytotoxicity. The biological study indicated that compounds 4-ethyl-5-(4,5,6,7-tetrahydro-1-benzothien-2-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 13, N-ethyl-5-(4,5,6,7-tetrahydro-1-benzothien-2-yl)-1,3,4-thiadiazol-2-amine 16, 4-amino-5-(4,5,6,7-tetrahydro-1-benzothien-2-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 20 and 4-amino-5-(5-phenylthien-2-yl)-2,4-dihydro-3H-1,2,4-triazole-3-thione 21 possessed high cytotoxicity in vitro against thymocytes. The corresponding IC50 values were 0.46 μM, 5.2 × 10−6 μM, 0.012 μM and 1.0 × 10−6 μM. Most toxic against lymphocytes was compound 21, IC50 – 0.012 μM. The tested compounds showed a general stimulation effect on B-cells' response.

Graphical abstractNovel derivatives of 4,5-substituted-1,2,4-triazole-3-thiones and 2,5-substituted-1,3,4-thiadiazoles were synthesized and evaluated for their cytotoxicity. High cytotoxicity was ascertained in test in vitro against thymocytes and lymphocytes and a general stimulating effect on B-cells' response.Figure optionsDownload full-size imageDownload as PowerPoint slide