SYNTHESIS OF SOME NOVEL 2-[5-MERCAPTO-3-(SUBSTITUED) [1,2,4] TRIAZOL-4-YL]-ISOINDOLE-1,3-DIONE DERIVATIVES AND EVALUATION OF THEIR ANTICANCER ACTIVITY ON EAC BEARING MICE MODEL

Author(s): Tanushree Singha Jagadish Singh, Jayatri Naskar, Tapan Kumar Maity* and Nimai Chand Ganguly

Abstract: Objective(s): A series of titled compounds were synthesized using conventional and microwave assisted fusion of phthalic anhydride moiety with mercaptotriazole via N-N bond. All the steps for synthesis have been done by conventional methods except the final step, which have been done also by microwave irradiation method for comparative study and in vivo anticancer activity was evaluated. Materials and Methods: In the present study six new isoindole-1,3-dione derivatives were synthesized. The structures of final synthesized compounds were assigned by using FT-IR, 1H NMR, LC-MS and their anticancer activity was evaluated on the Ehrlich Ascites Carcinoma (EAC) bearing Swiss albino mice model. Compounds were administered orally at dose of 100 mg/kg b.w. for 9 days. The effect of all the compounds on tumor growth inhibition was evaluated by studying the parameters such as tumor volume, percentage of the total cell count (viable and nonviable), the mean survival time, increasing life span and hematological parameters of the treated animal on nine groups of albino mice. Results: The result obtained confirms superiority of microwave irradiation method over conventional heating by increasing the yield value within a short period of reaction time. All compounds showed significant (P<0.01) anticancer activity compared to EAC control group and the compound 5e and 6e were found to be more potent. Conclusion: it can be concluded that isoindole-1,3-dione derivatives might have potent anticancer activity and microwave irradiation method was much better than traditional reflux method.

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