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真菌抗癌代谢产物:药物发现的合成研究

Fungal Anticancer Metabolites: Synthesis Towards Drug Discovery.

作者信息

Barbero Margherita, Artuso Emma, Prandi Cristina

机构信息

Department of Chemistry, University Degli Studi di Torino, via P. Giuria 7-10125 Torino, Italy.

出版信息

Curr Med Chem. 2018;25(2):141-185. doi: 10.2174/0929867324666170511112815.

Abstract

BACKGROUND

Fungi are a well-known and valuable source of compounds of therapeutic relevance, in particular of novel anticancer compounds. Although seldom obtainable through isolation from the natural source, the total organic synthesis still remains one of the most efficient alternatives to resupply them. Furthermore, natural product total synthesis is a valuable tool not only for discovery of new complex biologically active compounds but also for the development of innovative methodologies in enantioselective organic synthesis.

METHODS

We undertook an in-depth literature searching by using chemical bibliographic databases (SciFinder, Reaxys) in order to have a comprehensive insight into the wide research field. The literature has been then screened, refining the obtained results by subject terms focused on both biological activity and innovative synthetic procedures.

RESULTS

The literature on fungal metabolites has been recently reviewed and these publications have been used as a base from which we consider the synthetic feasibility of the most promising compounds, in terms of anticancer properties and drug development. In this paper, compounds are classified according to their chemical structure.

CONCLUSION

This review summarizes the anticancer potential of fungal metabolites, highlighting the role of total synthesis outlining the feasibility of innovative synthetic procedures that facilitate the development of fungal metabolites into drugs that may become a real future perspective. To our knowledge, this review is the first effort to deal with the total synthesis of these active fungi metabolites and demonstrates that total chemical synthesis is a fruitful means of yielding fungal derivatives as aided by recent technological and innovative advancements.

摘要

背景

真菌是治疗相关化合物,特别是新型抗癌化合物的著名且宝贵来源。尽管从天然来源分离很少能获得,但全有机合成仍然是重新供应这些化合物的最有效替代方法之一。此外,天然产物全合成不仅是发现新的复杂生物活性化合物的宝贵工具,也是对映选择性有机合成中创新方法发展的宝贵工具。

方法

我们通过使用化学文献数据库(SciFinder、Reaxys)进行了深入的文献检索,以便全面了解这个广泛的研究领域。然后对文献进行筛选,通过专注于生物活性和创新合成程序的主题词来完善所得结果。

结果

最近对有关真菌代谢物的文献进行了综述,这些出版物被用作基础,据此我们从抗癌特性和药物开发的角度考虑了最有前景化合物的合成可行性。在本文中,化合物根据其化学结构进行分类。

结论

本综述总结了真菌代谢物的抗癌潜力,强调了全合成的作用,概述了创新合成程序的可行性,这些程序有助于将真菌代谢物开发成可能成为真正未来前景的药物。据我们所知,本综述是首次对这些活性真菌代谢物的全合成进行探讨,并表明全化学合成是借助近期技术和创新进展产生真菌衍生物的富有成效的手段。

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