Evaluation of antitumor activity of novel triazole derivatives

In the present study, the three novel triazole derivatives (13c, 11b & 16c) were evaluated for their anti-tumor activity against Ehrlich Ascites Carcinoma (EAC) bearing Swiss albino mice. The test compounds were subjected for in-vitro preliminary cytotoxicity screening by trypan blue exclusion and MTT assay on cancer cell lines. In EAC ascites tumor model, the anti tumor activity of 13c, 11b and 16c was evaluated at the doses of 50mg/kg b.w by measuring the mean survival time, body weight changes, haematological parameters (WBC & RBC count and haemoglobin content) and cyclophosphamide was used as a standard. In addition, the effect of test compound on DNA was evaluated by DNA fragmentation assay. Among all the test compounds, 13c showed promising cytotoxic activity as compared to 11b and 16c when tested against cancer cell lines. In EAC model, the novel triazole compounds (13c, 11b and 16c) at a dose of 50mg/kg markedly enhanced the mean survival time of tumor bearing mice and activity was found more with compound 13c. The haematological parameters were also revealed anticancer activity of triazole derivatives whereas compound 13c has shown better activity when compared with other two compounds. In the mechanistic studies, the induction of apoptosis was confirmed by agarose gel electrophoresis and DNA binding studies revealed the binding efficacy of the compounds. From the present study it can be concluded that compound 13c has shown better anticancer activity when tested in-vitro and in-vivo than the 11b and 16c. However this study gives a lead for further research to establish the anticancer activity of these novel triazole derivatives.

Author(s): Bhavana V, Praveen Singh, Krishna KL and Purohit MN

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