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具有抗炎和抗癌作用的天然来源、半合成和合成分子。

Molecules of natural origin, semi-synthesis and synthesis with anti-inflammatory and anticancer utilities.

机构信息

REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia da Universidade Nova de Lisboa, 2829-516 Caparica, Portugal.

出版信息

Curr Pharm Des. 2012;18(26):3979-4046. doi: 10.2174/138161212802083644.

Abstract

The development of new drugs that can be valuable for the evolution of diseases' treatment is a goal for different areas of research, namely natural products chemistry, molecular biology and biochemistry, pharmacology, medicinal chemistry, synthetic organic chemistry and analytical chemistry. Nature is the main source of compounds for pharmaceutical purposes, either by providing the natural organic chemical compounds of interest or as a source of inspiration for the design of new drugs. The known anti-inflammatory and anticancer agents belong to a great diversity of structural skeletons since inflammatory and cancer processes involve many different biological targets. Their origins extend to plants, fungi, bacteria, and marine organisms, besides those produced by semi-synthesis and total synthesis. The tasks of the organic chemist are the screening, the structure assignment, and the semi and total syntheses of active molecules. Herein the screening and assignment of new active structures is addressed, together with other aspects, namely the improvements, both in availability and in effectiveness of action that can be achieved from new derivatives by synthetic or semi-synthetic strategies. Some aspects of drug delivery of anti-inflammatory and anticancer agents are considered. The bibliography presented is far from being exhaustive due to the prodigious number of published works. Instead, the most significant contributions in the scope of this review are described. The active compounds are organised by their biosynthetic origins as terpenoids; macrolides, polyketides and ansamycins; phenolics; alkaloids; peptides; glycoconjugates; other compounds, and food compounds.

摘要

开发可用于治疗疾病演变的有价值新药是不同研究领域的目标,包括天然产物化学、分子生物学和生物化学、药理学、药物化学、有机合成化学和分析化学。自然界是药物化合物的主要来源,它既可以提供有价值的天然有机化合物,也可以为新药设计提供灵感。已知的抗炎和抗癌药物属于多种多样的结构骨架,因为炎症和癌症过程涉及许多不同的生物靶标。它们的起源延伸到植物、真菌、细菌和海洋生物,以及半合成和全合成产物。有机化学家的任务是筛选、结构分配以及活性分子的半合成和全合成。本文重点介绍了新的活性结构的筛选和分配,以及其他方面,例如通过合成或半合成策略从新衍生物中获得的可用性和作用效果的提高。还考虑了抗炎和抗癌药物的药物传递的一些方面。由于发表的作品数量众多,因此呈现的文献远远不够详尽。相反,本文描述了这一综述范围内最显著的贡献。根据生物合成来源,将活性化合物分为萜类化合物;大环内酯、聚酮和安莎霉素;酚类;生物碱;肽;糖缀合物;其他化合物和食物化合物。

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