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Mini-Review Article

1- [4-（2-氨基乙氧基）苯基羰基] -3,5-双-（苄叉基）-4-哌啶酮类候选抗肿瘤药的发现和研究：我们近15年的研究

卷 28, 期 13, 2021

发表于: 30 July, 2020

页: [2453 - 2464] 页: 12

弟呕挨: 10.2174/0929867327666200730215752

价格: $65

摘要

这篇综述概述了我们的实验室在过去的15年中作为潜在药物候选物的一系列新的1- [4-2-氨基乙氧基）苯基羰基] -3,5-双-（亚苄基）-4-哌啶酮（5-8）的发现和开发。这些化合物中有许多表现出优异的细胞毒性，并且通常比当代抗癌药更有效。这些分子中许多的两个非常重要的特征是，第一，更大的肿瘤选择性毒性；第二，这些分子充当多药耐药性调节剂的能力。一些有效化合物的作用方式是通过凋亡诱导，活性氧的产生，某些胱天蛋白酶的活化以及影响线粒体功能。这些分子还显示出有希望的抗疟和抗分枝杆菌特性。在一项短期毒性研究中，这些分子在小鼠中具有良好的耐受性。已经提出了结构活性关系和药物递送系统以及这些化合物的药代动力学研究和代谢稳定性。与该系列（5-8）相关的积极特征值得进一步评估，以作为候选抗肿瘤药物候选物。

关键词: 哌啶酮，不饱和酮，姜黄素，抗癌，细胞毒性，抗疟疾，抗分枝杆菌，多药耐药性。

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