Synthesis and Evaluation of Antiproliferative activity of 1, 2, 4-Triazole Derivatives Against EAC Bearing Mice Model

Abstract:

A series of potential bioactive compounds, 4-Amino- 5-mercapto- 3-(4-chlorophenyl)-1, 2, 4-triazole (1d), 4-Amino- 5-mercapto- 3-(4-nitrophenyl)-1, 2, 4- triazole (2d) , 4-Amino- 5-mercapto-3-(2, 4-dichlorophenyl)-1, 2, 4-triazole (3d), 4-Amino- 5-mercapto- 3-(2-chlorophenyl)-1, 2, 4-triazole (4d), 4-Amino- 5- mercapto- 3-(2-methylphenyl)-1, 2, 4-triazole (5d), 4-Amino- 5-mercapto- , 2, 4-triazole (6d) were synthesized according to the literature methods. The synthesized compounds were characterized by FT-IR, 1H NMR spectroscopy, C H N analysis and anticancer activity was evaluated. Male Swiss albino mice has been used as test animal. Tumor cells used for anticancer activity were EAC (Ehrlich Ascites Carcinoma). Compounds were given at a dose of 25 mg/kg body weight intraperitoneally. groups were found to reduce tumor volume, viable cell count and increase the tumor weight (%) inhibition, ascites cells (%) inhibition and non-viable cell count and increase in life span (%ILS). All the compounds exhibited the significant (P< 0.01) anticancer activity compared to control and the compound 4d is found to be the most potent one. The standard drug was used as 5-Fluorouracil (20mg/kg, body weight).

Keywords: 1, 2, 4-triazole, anticancer activity, tumor cell count, tumor weight inhibition.