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

被引：70

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 07期

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

页码：2306 / 2310

页数：5

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