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首页> 外文期刊>Der Pharma Chemica: journal for medicinal chemistry, pharmaceutical chemistry and computational chemistry >Synthesis and Cytotoxicity of Novel Hexahydroquinoline-benzenesulfonamide Derivatives
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Synthesis and Cytotoxicity of Novel Hexahydroquinoline-benzenesulfonamide Derivatives

机译：新型六氢喹啉-苯磺酰胺衍生物的合成及细胞毒性

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The starting enamine derivatives 1a,c were allowed to react with different substituted benzylidenemalononitrile derivatives 2a,b to afford the corresponding tetrahydroquinoline-o-aminocarbonitrile derivatives 4a-d. The treatment of 4a-d with conc. H2SO4 at room temperature led to formation of hexahydroquinoline-oaminocarboxamide derivatives 5a-d, while complete hydrolysis had been occurred upon their refluxing with conc. H2SO4 to get the acid analogues 6a-d. Condensation reaction of the derivatives 4a-d with various acid chlorides in pyridine afforded the corresponding hexahydroquinoline-acetamide/benzamide derivatives 7a-d & 8a-d. Furthermore, the compounds 4a-d were fused with urea, thiourea, formamide and acetic anhydride to gain the novel hexa(tetra)hydropyrimido[4,5-b]quinolin derivatives 9a-d, 10a-d, 11a-d and 12a-d, respectively. Some of the newly synthesized analogues were chosen to evaluate their in-vitro cytotoxic activity against human liver carcinoma cell lines (HEPG2). The obtained data revealed that the tested derivatives produced significant activity in comparison with the used reference drug Doxorubicin.
机译：使起始烯胺衍生物1a，c与不同的取代的亚苄基丙二腈衍生物2a，b反应，得到相应的四氢喹啉-o-氨基腈衍生物4a-d。 4a-d浓度的治疗。室温下的硫酸导致六氢喹啉-氨基氨基甲酰胺衍生物5a-d的形成，而在与浓盐酸回流时发生了完全水解。用H 2 SO 4得到酸类似物6a-d。衍生物4a-d与各种酰氯在吡啶中的缩合反应得到相应的六氢喹啉-乙酰胺/苯甲酰胺衍生物7a-d和8a-d。此外，将化合物4a-d与尿素，硫脲，甲酰胺和乙酸酐融合以获得新的六（四）氢嘧啶基[4,5-b]喹啉衍生物9a-d，10a-d，11a-d和12a- d，分别。选择一些新合成的类似物以评估其对人肝癌细胞系（HEPG2）的体外细胞毒活性。获得的数据表明，与使用的参考药物阿霉素相比，所测试的衍生物产生了显着的活性。

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