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Publication Type : Journal Article
Publisher : Medicinal Chemistry Research
Source : Medicinal Chemistry Research, Volume 22, Issue 8, p.3911 - 3917 (2013)
Campus : Kochi
School : School of Pharmacy
Department : Pharmaceutical Chemistry & Analysis
Year : 2013
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 ED50value 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.
Cite this Research Publication : Bijo Mathew, Suresh, J., and 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”, Medicinal Chemistry Research, vol. 22, no. 8, pp. 3911 - 3917, 2013.