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乙内酰脲、硫代乙内酰脲和硒代乙内酰脲作为抗癌剂的最新进展:构效关系与设计策略

Recent Development in Hydantoins, Thiohydantoins, and Selenohydantoins as Anticancer Agents: Structure-activity Relationship and Design Strategies.

作者信息

Gupta Ajay Kumar, Thakur Gajendra Singh, Jain Sanmati Kumar

机构信息

Drug Discovery and Research Laboratory, Department of Pharmacy, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur, 495009, Chhattisgarh, India.

出版信息

Mini Rev Med Chem. 2025;25(9):693-726. doi: 10.2174/0113895575329643241206101210.

Abstract

Hydantoin, a five-membered heterocyclic scaffold, is regarded as a crucial scaffold in medicinal chemistry. Hydantoins have been useful in synthesizing medicines like nilutamide, enzalutamide, and apalutamide. Thiohydantoin and selenohydantoin have been discovered as two separate types of hydantoin. There are two hydrogen bond donors, two hydrogen bond acceptors, and four substitution sites. These characteristics have led to the design, synthesis, and expansion of hydantoin derivatives' biological and pharmacological effects against numerous types of malignancies. This study reviews the recent contributions of hydantoin and its isosteric variants to medicinal chemistry. To emphasize their significance, certain significant compounds based on hydantoins and their structure activity relationships (SAR) are briefly discussed. We thoroughly analyzed each scaffolds' structural characteristics and SAR, and these scaffolds may one day show potential anticancer activities.

摘要

乙内酰脲是一种五元杂环骨架,被认为是药物化学中的关键骨架。乙内酰脲在合成诸如尼鲁米特、恩杂鲁胺和阿帕鲁胺等药物方面很有用。硫代乙内酰脲和硒代乙内酰脲已被发现是乙内酰脲的两种不同类型。有两个氢键供体、两个氢键受体和四个取代位点。这些特性导致了乙内酰脲衍生物针对多种类型恶性肿瘤的生物学和药理作用的设计、合成及扩展。本研究综述了乙内酰脲及其等排变体对药物化学的最新贡献。为强调它们的重要性,简要讨论了某些基于乙内酰脲的重要化合物及其构效关系(SAR)。我们全面分析了每个骨架的结构特征和SAR,这些骨架未来可能会展现出潜在的抗癌活性。

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