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

被引：0
作者：
Bijo Mathew
Jerad Suresh
Devaraji Vinod
机构：
[1] Grace College of Pharmacy,Department of Pharmaceutical Chemistry
[2] Madras Medical College,Department of Pharmaceutical Chemistry
来源：
Medicinal Chemistry Research | 2013年 / 22卷
关键词：
Alanine amino transferase; Alkaline phosphatase; Aspartate amino transferase; Barbituric acid; Knoevenagel condensation; Total cholesterol;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
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 ED50 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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页码：3911 / 3917
页数：6
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