摘要
本文综述了螺环化合物的药物化学研究进展,该化合物是一类更广泛的天然和合成有机分子,被定义为两个分子实体的杂化物cova。以独特的四面体碳连接。这种Spiro中心碳为分子提供了一个三维结构取向的框架,在许多与医学相关的化合物中都有这种结构。s,一个众所周知的例子是抗高血压螺内酯.各种生物活性天然产物具有特殊的Spiro连锁,其不同的化学类型成为综合利用的材料。e自20世纪以来。事实上,已经有越来越多的兴趣,在合成杂环杂化收集通过一个斯皮罗碳。这些组合中的大多数是一个脚手架中的两个单元。能够通过顺序机制干扰生物系统。含有吲哚或吲哚单元的螺环杂种是与生物受体相互作用较强的化合物。通过蛋白质抑制或酶途径的TOR及其在靶向化疗中被认为是有前景的抗癌药物是可以预见的。这些特殊的、低重量和非复杂的螺环杂种S是SIRT 1、MDM2-p53和Plk 4的有效抑制剂,对间变性淋巴瘤激酶(ALK)受体具有亲和力。它们也被称为优秀的dna结合剂,作用于细胞分裂。细胞周期处于不同阶段,诱导凋亡细胞死亡。螺环杂种的结构多样性已证明具有神经保护作用、抗艾滋病病毒、抗病毒和抗菌活性。领带。在这篇综述中提到了上百篇论文,其中包括一些潜在的化学问题和Spiro化合物的药效学效力,这使得它们在创新药物的冲击下令人印象深刻。支票电托收,象征式互动.
关键词: 螺环化合物,杂环,杂合物,合成,生物活性,药物设计,抗癌,抑制作用。
Current Medicinal Chemistry
Title:Advances in Spirocyclic Hybrids: Chemistry and Medicinal Actions
Volume: 25 Issue: 31
关键词: 螺环化合物,杂环,杂合物,合成,生物活性,药物设计,抗癌,抑制作用。
摘要: The present review deals with the progress in medicinal chemistry of spirocyclic compounds, a wider class of natural and synthetic organic molecules, defined as a hybrid of two molecular entities covalently linked via a unique tetrahedral carbon. This spiro central carbon confers to the molecules a tridimensional structurally oriented framework, which is found in many medicinally relevant compounds, a well-known example is the antihypertensive spironolactone. Various bioactive natural products possess the privileged spiro linkage and different chemo-types thereof become synthetically accessible since the 20th century. Actually, there has been a growing interest in the synthesis of heterocyclic hybrids gathered via a spiro carbon. Most of these combinations are two moieties in one scaffold being able to interfere with biological systems through sequential mechanisms. Spirocyclic hybrids containing indole or oxindole units are compounds exhibiting higher interaction with biological receptors by protein inhibition or enzymatic pathways and their recognition as promising anticancer agents in targeted chemotherapy is foreseen. These specific, low-weight and noncomplex spirocyclic hybrids are potent inhibitors of SIRT1, Mdm2–p53 and PLK4, showing affinity for anaplastic lymphoma kinase (ALK) receptor. They are also known as excellent DNA binders, acting on cellular division by arresting the cell cycle at different phases and inducing apoptotic cell death. A structural diversity of spirocyclic hybrids has proved neuroprotective effects, anti-HIV, antiviral and antibacterial activities. Hundred of papers are mentioned in this review underlying chemical issues and pharmacological potencies of spiro compounds, which render them impressive synthetic hits for innovative drug conception.
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Cite this article as:
Advances in Spirocyclic Hybrids: Chemistry and Medicinal Actions, Current Medicinal Chemistry 2018; 25 (31) . https://dx.doi.org/10.2174/0929867325666180309124821
DOI https://dx.doi.org/10.2174/0929867325666180309124821 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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