<br>均三嗪核心化合物生物活性的最新进展,Pharmaceuticals

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均三嗪核心化合物生物活性的最新进展
Pharmaceuticals ( IF 4.286 ) Pub Date : 2022-02-14 , DOI: 10.3390/ph15020221
Dawid Maliszewski ₁ , Danuta Drozdowska ₁

Affiliation

成功化疗的有效策略依赖于创造与正常细胞相比对癌细胞具有高选择性且细胞毒性相对较低的化合物。其中一种方法是发现癌细胞中的关键点，即产生潜在治疗靶标的特定酶的地方。三嗪是苯环结构中三个氮取代碳氢单元的六元杂环化合物。本综述的主题是对称的 1,3,5-三嗪，称为 s-三嗪。 1,3,5-三嗪是最古老的杂环化合物之一。由于其低成本和高可用性，其新颖的合成方法引起了研究人员的关注。 s-三嗪具有弱碱，其共振能量比苯弱得多，因此，亲核取代优于亲电取代。具有对称均三嗪核心的杂环代表一类有趣的化合物，其具有广泛的生物特性，例如抗癌、抗病毒、杀真菌、杀虫、杀菌、除草和抗微生物、抗疟剂。它们还可以用作染料、润滑剂和分析试剂。因此，1,3,5-三嗪衍生物组已发展多年。三嗪不仅是其中的核心，而且是提高整个衍生物动能的因素。修饰结构和引入新的取代基使得获得对增殖等过程具有广泛抑制活性的化合物成为可能。在一些情况下，均三嗪衍生物诱导细胞凋亡。在这篇综述中，我们将介绍目前研究的具有抗癌活性的 1,3,5-三嗪衍生物，特别强调它们对肿瘤发生过程中涉及的酶的抑制作用。

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Recent Advances in the Biological Activity of s-Triazine Core Compounds

An effective strategy for successful chemotherapy relies on creating compounds with high selectivity against cancer cells compared to normal cells and relatively low cytotoxicity. One such approach is the discovery of critical points in cancer cells, i.e., where specific enzymes that are potential therapeutic targets are generated. Triazine is a six-membered heterocyclic ring compound with three nitrogen replacing carbon-hydrogen units in the benzene ring structure. The subject of this review is the symmetrical 1,3,5-triazine, known as s-triazine. 1,3,5-triazine is one of the oldest heterocyclic compounds available. Because of its low cost and high availability, it has attracted researcher attention for novel synthesis. s-Triazine has a weak base, it has much weaker resonance energy than benzene, therefore, nucleophilic substitution is preferred to electrophilic substitution. Heterocyclic bearing a symmetrical s-triazine core represents an interesting class of compounds possessing a wide spectrum of biological properties such as anti-cancer, antiviral, fungicidal, insecticidal, bactericidal, herbicidal and antimicrobial, antimalarial agents. They also have applications as dyes, lubricants, and analytical reagents. Hence, the group of 1,3,5-triazine derivatives has developed over the years. Triazine is not only the core amongst them, but is also a factor increasing the kinetic potential of the entire derivatives. Modifying the structure and introducing new substituents makes it possible to obtain compounds with broad inhibitory activity on processes such as proliferation. In some cases, s-triazine derivatives induce cell apoptosis. In this review we will present currently investigated 1,3,5-triazine derivatives with anti-cancer activities, with particular emphasis on their inhibition of enzymes involved in the process of tumorigenesis.

更新日期：2022-02-14

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