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首页> 外文期刊>Current Science: A Fortnightly Journal of Research >Synthesis, heterocyclization and anti-tumour activity evaluation of some benzimidazole derivatives
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Synthesis, heterocyclization and anti-tumour activity evaluation of some benzimidazole derivatives

机译：一些苯并咪唑衍生物的合成，杂环化和抗肿瘤活性评价

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摘要

Methylbenzimidazole 1 is converted to imidazole acrylic acid 3 via cyclo condensation with chloral followed by hydrolysis. Compound 3 also obtained from the reaction of o-phenylenediamine with maleic anhydride. Treatment of 1 with SeO2 yielded the oxidized product 4 (Aldehyde 4) which undergoes Wittig reaction using ester and Ph3P to furnish the acrylates 5. Compound 5 is also obtained by cyclocondensation of o-phenylenediamine and the corresponding maleate. Cyclization of 3 using Ac2O provides pyrroloimidazole 6. Imidazole 6 undergoes several transformations using HCI, ammonium hydroxide in neutral medium, o-phenylene diamine/HCI to provide acrylic acid 3, amide 7 and/or bicompound 8 respectively. Anilide 9 is obtained as a result of condensation of 3 with amines. Ester 5 undergoes 1,4-addition to benzimidazole ring to give the corresponding anilino derivative 10. Pyridazine cyclization is acheived by treatment of 5 with NH2OH in acidic medium. In vitro cytotoxicity is evaluated using SRB (sulphorhodamine-B) assay against two human cell lines, breast and liver carcinoma cell lines. The results show that compound 11 has strong activity against all cell lines tested.
机译：通过用氯的环缩合将甲基苯并咪唑1转化为咪唑丙烯酸3，然后用水解。化合物3还从O-苯二胺与马来酸酐的反应得到的。用SEO 2处理1，得到氧化产物4（醛4），其使用酯和pH3p进行诸如丙烯酸酯的丙烯酸酯5。化合物5也通过O-苯二胺的环核和相应的马来酸酯获得。 3使用AC2O的环化提供吡咯莫咪唑6.咪唑6经历使用HCl，中性介质中的氢氧化铵，O-苯基二胺/ HCl的几种转化，分别提供丙烯酸3，酰胺7和/或双组合8。作为3用胺的缩合而获得苯lidide9。酯5经历1,4-除苯并咪唑环，得到相应的苯胺砜衍生物10.通过在酸性培养基中处理5，通过用NH 2 OH处理5来实现吡啶啶环化。使用SRB（Sulphorhodamine-B）测定对两种人细胞系，乳腺癌和肝癌细胞系评估体外细胞毒性。结果表明，化合物11对测试的所有细胞系具有很强的活性。

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