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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and structure-activity relationship study of 8-hydroxyquinoline-derived Mannich bases as anticancer agents.
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Synthesis and structure-activity relationship study of 8-hydroxyquinoline-derived Mannich bases as anticancer agents.

机译：8-羟基喹啉衍生的曼尼希碱作为抗癌剂的合成及构效关系研究。

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摘要

To continue our early study on the structural modifications of clioquinol, more 8-hydroxyquinoline-derived Mannich bases were synthesized and examined for growth-inhibitory effect. Taken Mannich base 1 as our lead compound, upon replacement of either sulfonyl group with methylene group or piperazine ring with ethylenediamine group resulted in an appreciable increase in potency. On the other hand, as 8-hydroxyquinoline was replaced with phenol, 3-hydroxypyridine and 1-naphthol, a dramatic decrease in activity was observed, indicating that 8-hydroxyquinoline is a crucial scaffold for activity. Further 3D-QSAR analysis on HeLa cells revealed that both steric and electronic effects contributed equally to growth inhibition. Taken together, the structure-activity relationships obtained from both in vitro data and CoMFA model warrant a valuable reference for further study.
机译：为了继续我们对氯喹醇的结构修饰的早期研究，合成了更多的8-羟基喹啉衍生的曼尼希碱，并检查了其抑制生长的作用。以曼尼希碱1为先导化合物，用亚甲基取代磺酰基或用乙二胺基取代哌嗪环后，效力显着提高。另一方面，当用酚，3-羟基吡啶和1-萘酚代替8-羟基喹啉时，观察到活性急剧降低，表明8-羟基喹啉是活性的关键支架。对HeLa细胞的进一步3D-QSAR分析显示，空间效应和电子效应均对生长抑制起同样作用。两者合计，从体外数据和CoMFA模型获得的结构活性关系值得进一步研究的宝贵参考。

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