卤素基喹唑啉-4(3H)-酮衍生物作为 MCF-7 乳腺癌抑制剂:目前的发展和结构-活性关系。

IF 4.3 3区 医学 Q2 CHEMISTRY, MEDICINAL Archiv der Pharmazie Pub Date : 2024-11-13 DOI:10.1002/ardp.202400740
Rachana Upadhyay, Pooja Tandel, Amit B Patel
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引用次数: 0

摘要

目前,癌症是一项严重的健康挑战,其发病率超出了限制范围。乳腺癌仍然是导致妇女癌症相关发病率和死亡率的主要因素之一。化疗仍然是治疗各种癌症的关键。目前有几种抗肿瘤药物正处于不同的临床试验阶段,还有更多的药物已被批准用于临床。然而,这些药物有可能产生不良反应,某些人还可能对这些药物产生抗药性,从而最终降低药物的疗效。因此,发现、开发和改进有可能抑制增殖途径的新型抗癌药物分子至关重要。近年来,喹唑啉酮衍生物,特别是卤素取代的 4(3H)-喹唑啉酮,作为一类前景广阔的新型化疗药物引起了人们的关注。此外,在对 MCF-7 细胞系进行体外测试时,这些分子在微摩尔范围内显示出显著的抑制作用。因此,本研究旨在强调卤原子引人入胜的多功能性,深入总结并重点介绍卤代 4(3H)-喹唑啉酮类化合物抗癌特性的最新进展。书中还详细讨论了各种官能团的结构-活性关系(SAR),以及通过分子对接研究了解它们与氨基酸残基的相互作用。其目的是促进新发现,从而激发该领域的创新研究。因此,本研究通过延长药理活性候选药物的阵列来简化药物设计和开发策略。
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Halogen-based quinazolin-4(3H)-one derivatives as MCF-7 breast cancer inhibitors: Current developments and structure-activity relationship.

Currently, cancer is a serious health challenge with predominance beyond restrictions. Breast cancer remains one of the major contributors to cancer-related morbidity and mortality in women. Chemotherapy continues to be crucial in the treatment of all variants of cancer. Several antitumor drugs are presently in different phases of clinical trials, whereas many more have been approved for clinical use. However, these drugs have the potential to cause adverse effects, and certain individuals may become resistant to them, which would eventually reduce the drug's efficacy. Therefore, it is essential to discover, develop, and improve newer anticancer drug molecules that could potentially inhibit proliferative pathways. In recent years, quinazolinone derivatives, more specifically halogen-substituted 4(3H)-quinazolinone, have drawn attention as a promising new class of chemotherapeutic agents. In addition, these molecules showed significant inhibition in micromolar ranges when tested in vitro against the MCF-7 cell line. Therefore, this study aims to emphasize the intriguing versatility of halogen atoms, providing an in-depth summary and highlighting recent developments in the anticancer properties of halogenated 4(3H)-quinazolinones. It also features a detailed discussion of the structure-activity relationship (SAR) of various functional groups and their interaction with amino acid residues utilizing molecular docking studies. The intent is to foster novel discoveries that can inspire innovative investigations in this domain. Hence, this study simplifies the drug design and development strategies by prolonging the array of pharmacologically active candidates.

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来源期刊
Archiv der Pharmazie
Archiv der Pharmazie 医学-化学综合
CiteScore
7.90
自引率
5.90%
发文量
176
审稿时长
3.0 months
期刊介绍: Archiv der Pharmazie - Chemistry in Life Sciences is an international journal devoted to research and development in all fields of pharmaceutical and medicinal chemistry. Emphasis is put on papers combining synthetic organic chemistry, structural biology, molecular modelling, bioorganic chemistry, natural products chemistry, biochemistry or analytical methods with pharmaceutical or medicinal aspects such as biological activity. The focus of this journal is put on original research papers, but other scientifically valuable contributions (e.g. reviews, minireviews, highlights, symposia contributions, discussions, and essays) are also welcome.
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