Cancer is one of the leading causes of death worldwide in spite of the immense efforts in the search for effective anti-cancer drugs. Triazoles are the class of heterocyclic compounds which has a wide variety of activity, low toxicity and good Pharmacokinetic and Pharmacodynamics profiles. The present study was aims to investigate the anti-tumor activity of the novel 1,2,4 triazole derivatives (viz., MPA and OBC) which were synthesized in Dept. of Chemistry laboratory, JSS College of Pharmacy, Mysore. The compounds were subjected for in vitro cytotoxicity studies like – Sulforhodamine B assay and DNA fragmentation assay further the compounds were evaluated for anti-tumor activity against Erhlich Ascite Carcinoma (EAC) and Dalton Lymphoma Ascites (DLA) induced tumours in Swiss Albino Mice. In EAC model, anti-tumor activity was evaluated by change in body weight, mean survival time and hematological parameters. In DLA model, tumor volume and tumor weight was evaluated. Acute toxicity studies of MPA and OBC were done according to OECD – 423 guidelines and were found to be safe at 300 mg/kg. Both the compounds showed good cytotoxic potential by in-vitro cytotoxicity assays. The novel 1,2,4 triazole derivatives was found to possess the antitumor activity on liquid and solid tumor model which is very much nearer to the standard group. However, further detail research is required to establish anti-tumor activity of novel 1,2,4 triazole derivatives.