Abstract
A new series of novel benzimidazole derivatives containing barbitone moiety (5a–f) was synthesized by a Knoevenagel condensation of (2E)-1-(1H-benzimidazol-2-yl)-3-phenylprop-2-en-1-ones (4a–f) and barbituric acid in the presence of catalytic amount of acetic acid medium. All the final structures were assigned on the basis of IR, 1H NMR and mass spectra analysis. Acute toxicity studies were performed initially to determine the safety of titled derivatives and the ED 50 value was calculated 50 mg/kg. All the final derivatives were screened for antitumour activity against Dalton’s ascitic lymphoma in mice. All the new candidates at a dose of 50 mg/kg showed a good antitumour activity against DLA-bearing mice when compared to the standard 5-fluro uracil. Among the final derivatives (5e), 5-[(2E)-1-(1H-benzimidazol-2-yl)-3-(3-nitrophenyl) prop-2-en-1-ylidene] pyrimidine-2,4,6(1H,3H,5H)-trione was found to be most potent antitumour in nature.
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Acknowledgments
The authors are highly thankful to Dr. N. Chidhambarnathan, K.M.College of Pharmacy, Madurai, India, Mrs. Githa Elizabeth Mathew, Assistant Professor, Department of pharmacology, Grace College of Pharmacy, Kerala, India, for carrying out the pharmacological work for the present study. Authors also acknowledge the help of Dr. N. Murugesan, SAIF IIT, Chennai, for carrying out the spectral analysis
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Mathew, B., Suresh, J. & Vinod, D. Antitumour activity of 5-[(2E)-1-(1H-benzimidazol-2-yl)-3-substituted phenylprop-2-en-1-ylidene] pyrimidine-2,4,6(1H,3H,5H)-triones against Dalton’s ascitic lymphoma in mice. Med Chem Res 22, 3911–3917 (2013). https://doi.org/10.1007/s00044-012-0407-1
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DOI: https://doi.org/10.1007/s00044-012-0407-1