Department of Chemistry, Indian Institute of Technology-Roorkee, Roorkee 247 667 UK, India.
Bioorg Med Chem Lett. 2010 Apr 1;20(7):2306-10. doi: 10.1016/j.bmcl.2010.01.147. Epub 2010 Feb 2.
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 p.o. compounds 3b (39.4%) and 3c (39.2%) exhibited anti-inflammatory activity, comparable to standard ibuprofen which showed 39% activity at 50 mg/kg p.o. and compound 7c exhibit good anticancer activity against ovary (IGR-OV-1), breast (MCF-7) and CNS(SF-295) human cancer cell lines.
通过缩合琥珀酸（1）、均苯四甲酸（4）和 2,3- 哒嗪二羧酸（6）与各种取代二胺，在微波辐射下合成了杂环苯并咪唑衍生物 3a-h、5a-c 和 7a-d，产率较高。3a-h、5a-c 和 7a-d 的结构均由光谱数据充分证实。所有这些化合物均进行了抗炎和抗癌活性筛选。在 50mg/kg 口服剂量下，化合物 3b（39.4%）和 3c（39.2%）表现出抗炎活性，与标准布洛芬（50mg/kg 口服时活性为 39%）相当，而化合物 7c 对卵巢（IGR-OV-1）、乳腺（MCF-7）和中枢神经系统（SF-295）人癌细胞系表现出良好的抗癌活性。
