Solvent free synthesis, anti-inflammatory and anticancer activity evaluation of tricyclic and tetracyclic benzimidazole derivatives

被引:69
|
作者
Sondhi, Sham M. [1 ]
Rani, Reshma [1 ]
Singh, Jaiveer [1 ]
Roy, Partha [2 ]
Agrawal, S. K. [3 ]
Saxena, A. K. [3 ]
机构
[1] Indian Inst Technol Roorkee, Dept Chem, Roorkee 247667, Uttar Pradesh, India
[2] Indian Inst Technol Roorkee, Dept Biotechnol, Roorkee 247667, Uttar Pradesh, India
[3] Indian Inst Integrat Med, Div Pharmacol, Jammu 180001, India
关键词
Benzimidazole; Heterocyclic; Anti-inflammatory; Anticancer; Microwave; KINASE; TRYPTANTHRIN; INHIBITORS; ALKALOIDS; PRODUCTS; ANALOGS; ASSAY;
D O I
10.1016/j.bmcl.2010.01.147
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Heterocyclic benzimidazole derivatives 3a-h, 5a-c and 7a-d have been synthesized by condensation of succinic acid (1) homophthalic acid (4) and 2,3-pyrazinedicarboxlic acid (6) with various substituted diamines under microwave irradiation in good yields. Structures assigned to 3a-h, 5a-c and 7a-d are fully supported by spectral data. All these compounds were screened for anti-inflammatory and anticancer activities. At a dose of 50 mg/kg po compounds 3b (39.4%) and 3c (39.2%) exhibited anti-inflammatory activity, comparable to standard ibuprofen which showed 39% activity at 50 mg/kg po and compound 7c exhibit good anticancer activity against ovary (IGR-OV-1), breast (MCF-7) and CNS(SF-295) human cancer cell lines. (C) 2010 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2306 / 2310
页数:5
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