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美国食品药品监督管理局(FDA)批准的用于癌症治疗的杂环分子:合成、剂量、作用机制及其不良反应。

FDA-approved heterocyclic molecules for cancer treatment: Synthesis, dosage, mechanism of action and their adverse effect.

作者信息

Hossain Mossaraf, Habib Imran, Singha Koustav, Kumar Anoop

机构信息

Synthetic Organic Research Laboratory, UGC-HRDC (Chemistry), University of North Bengal, Darjeeling, 734013, India.

Department of Biotechnology, University of North Bengal, Darjeeling, 734013, India.

出版信息

Heliyon. 2023 Dec 5;10(1):e23172. doi: 10.1016/j.heliyon.2023.e23172. eCollection 2024 Jan 15.

Abstract

As the incorporation of heterocycles increases the physical characteristics and biological activity of pharmacological molecules, heterocyclic scaffolds are commonly discovered as common cores in a wide spectrum of biologically active drugs. In the contemporary context, many heterocycles have arisen, playing vital roles in diverse pharmaceutical compounds that benefit humanity. Over 85 % of FDA-approved medication molecules contain heterocycles, and most importantly, numerous heterocyclic medicinal molecules indicate potential benefits against a range: of malignancies. The unique flexibility and dynamic core scaffold of these compounds have aided anticancer research. These medications are used to treat cancer patients by targeting particular genes, enzymes, and receptors. Aside from the drugs that are now on the market, numerous forms are being researched for their potential anti-cancer activity. Here in this review, we classified some molecules and biologically active heterocycles containing anticancer medicinal moieties approved by the FDA between 2019 and 2021 based on their use in various forms of cancer. We will focus on those that are suitable for cancer treatment, as well as the essential biochemical mechanisms of action, biological targets, synthetic methods, and inherent limiting considerations in their use.

摘要

由于杂环的引入会增加药理分子的物理特性和生物活性,因此杂环骨架在广泛的生物活性药物中通常被发现是常见的核心结构。在当代背景下,许多杂环已经出现,在造福人类的各种药物化合物中发挥着至关重要的作用。超过85%的FDA批准的药物分子含有杂环,最重要的是,许多含杂环的药物分子显示出对一系列恶性肿瘤的潜在益处。这些化合物独特的灵活性和动态核心骨架有助于抗癌研究。这些药物通过靶向特定的基因、酶和受体来治疗癌症患者。除了目前市场上的药物外,许多形式的药物正在研究其潜在的抗癌活性。在这篇综述中,我们根据2019年至2021年间FDA批准的含抗癌药物部分的一些分子和生物活性杂环在各种癌症中的用途进行了分类。我们将重点关注那些适合癌症治疗的药物,以及其基本的生化作用机制、生物靶点、合成方法及其使用中固有的限制因素。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/23a4/10755292/776d05e767b4/gr1.jpg

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