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Review Article

近年来DHFR抑制剂作为抗癌药物修饰的设计和构效关系研究

卷 28, 期 5, 2021

发表于: 16 October, 2019

页: [910 - 939] 页: 30

弟呕挨: 10.2174/0929867326666191016151018

价格: $65

摘要

背景：二氢叶酸还原酶(DHFR)几十年来一直被认为是抗菌、抗真菌和抗疟疾治疗的分子靶点。这种酶在新的抗癌药物的设计中变得越来越重要，这已被许多研究证实，包括建模、合成和体外生物研究。本文旨在介绍和讨论具有潜在抗癌活性的新型DHFR抑制剂的研究进展。 方法：过去十年关于DHFR抑制剂的不同类型的科学文献已经被搜索。综述了近年来国内外在设计、合成和构效关系研究方面的研究进展，并根据先导分子及其结构修饰的不同将其划分为几个小领域。介绍了新化合物DHFR抑制剂的各种合成方法、潜在的抗癌活性和可能的实际应用。 结果：本文综述了目前已知的DHFR抑制剂的修饰和80个新分子的结构和寻找，这些新分子被设计为有潜力的抗癌药物。此外，本文还介绍了作用于胸腺酸合成酶(TS)、碳酸酐酶(CA)甚至DNA结合的DHFR抑制剂。 结论：深入的物理化学表征和生物研究突出了DHFR抑制剂的构效关系。这将有助于更好地设计和合成活性化合物，使其具有预期的作用机理和预期的活性。

关键词: 二氢叶酸还原酶(DHFR)，甲氨蝶呤，甲氧苄氨嘧啶，抗癌药物，胸腺嘧啶合酶(TS)，药物设计，叶酸代谢

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