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Pyrazoline bearing benzimidazoles: search for anticancer agent.

机译:吡唑啉轴承苯并咪唑:寻找抗癌剂。

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摘要

2-acetyl benzimidazole was allowed to react with substituted aromatic aldehydes to get desired intermediate chalcones (2a-g), the cyclocondensation of these intermediates with hydrazine hydrate and phenyl hydrazine in two separate reactions yielded pyrazoline derivatives (3a-g &4a-g respectively). Among the synthesize compounds, six compounds were granted NSC code and screened at National Cancer Institute (NCI), USA for anticancer activity at a single high dose (10(-5) M) in full NCI 60 cell panel. Among the selected compounds, (4f) 2-[5-(3,4-dimethoxyphenyl)-1-phenyl-4,5-dihydro-1H-3-pyrazolyl]-1H-benzimidazole (NSC 748326) was found to be the most active candidate of the series and selected for further evaluation at five dose level screening.
机译:使2-乙酰基苯并咪唑与取代的芳族醛反应以获得所需的中间丘酮(2A-G),将这些中间体与肼水合物和苯基肼在两个单独的反应中产生的环干化产生吡唑啉衍生物(分别为3A-G和4A-G) 。 在合成化合物中,六种化合物被授予NSC代码,并在全国癌症研究所(NCI),美国,用于全NCI 60细胞面板中的单一高剂量(10(-5)m)的抗癌活性。 在选定的化合物中,(4F)2- [5-(3,4-二甲氧基苯基)-1-苯基-4,5-二氢-1H-3-吡唑基] -1H-苯并咪唑(NSC 748326)是 该系列最活跃的候选者,并在五种剂量水平筛选中选择进一步评估。

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