摘要
考虑到癌症仍然是世界范围内的重要死亡原因,几种常规的抗癌治疗被广泛使用。然而,它们中的大多数对恶性细胞表现出低选择性并引起许多不良副作用。其中,使用基于 5-氟尿嘧啶 (5-FU) 的疗法是最有效的疗法之一,具有广谱性。由于这些情况,已经开发了 5-FU 的各种改进,以改善药物输送并减少副作用。在优化策略中,对 N1 或 N3 位置的 5-FU 进行修饰,通常包括掺入具有抗癌活性的药理活性化合物(称为杂化分子)和与其他化合物组(称为缀合物)的功能化。已经进行了几项研究,以寻找针对癌症的新替代疗法。他们中的许多人已经证明,杂化化合物表现出良好的抗癌活性,这已成为该药物发现和开发领域的一个有前途的策略。此外,5-FU 与氨基酸、肽、磷脂、聚合物等的结合可提高代谢稳定性和吸收。本综述强调了基于 5-FU 的杂交体和衍生物作为开发抗肿瘤药物支架的潜力。此外,它还详细描述了用于设计和合成这些化合物的不同策略,以及它们的生物活性和构效关系 (SAR) 分析。
关键词: 5-氟尿嘧啶、癌症、抗癌活性、混合化合物、共轭物、构效关系 (SAR)。
Current Medicinal Chemistry
Title:Chemistry and Anticancer Activity of Hybrid Molecules and Derivatives based on 5-Fluorouracil
Volume: 28 Issue: 27
关键词: 5-氟尿嘧啶、癌症、抗癌活性、混合化合物、共轭物、构效关系 (SAR)。
摘要:
Considering that cancer continues to be an important cause of death worldwide, several conventional anticancer treatments are widely used. However, most of them display low selectivity against malignant cells and induce many adverse side effects. Among these, the use of therapies based on 5-Fluorouracil (5-FU) has been one of the most efficient, with a broad-spectrum. Due to these circumstances, various modifications of 5-FU have been developed to improve drug delivery and reduce side effects. Among the optimization strategies, modifications of 5-FU at N1 or N3 position are made, usually including the incorporation of pharmacologically active compounds with anticancer activity (called hybrid molecule) and functionalization with other groups of compounds (called conjugates).
Several studies have been conducted in the search for new alternative therapies against cancer. Many of them have evidenced that hybrid compounds exhibit good anticancer activity, which has emerged as a promising strategy in this field of drug discovery and development. Furthermore, the binding of 5-FU to amino acids, peptides, phospholipids, polymers, among others, improves metabolic stability and absorption.
This review highlights the potential of hybrids and derivatives based on 5-FU as a scaffold for the development of antitumor agents. Besides, it also presents a detailed description of the different strategies employed to design and synthesized these compounds, together with their biological activities and structure-activity relationship (SAR) analysis.
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Cite this article as:
Chemistry and Anticancer Activity of Hybrid Molecules and Derivatives based on 5-Fluorouracil, Current Medicinal Chemistry 2021; 28 (27) . https://dx.doi.org/10.2174/0929867328666210211164314
DOI https://dx.doi.org/10.2174/0929867328666210211164314 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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