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吲哚衍生物作为抗癌剂的最新研究进展:一种基于机制的方法。

Recent Development in Indole Derivatives as Anticancer Agent: A Mechanistic Approach.

机构信息

Laboratory of Natural Products, Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Bathinda (Pb), 151001, India.

出版信息

Anticancer Agents Med Chem. 2021;21(14):1802-1824. doi: 10.2174/1871520621999210104192644.

Abstract

BACKGROUND

Cancer accounts for several deaths each year. There are multiple FDA approved drugs for cancer treatments. Due to the severe side effects and multiple drug resistance, the current drug therapies become ineffective. So, the newer moieties with fewer toxic effects are necessary for the development.

OBJECTIVE

The mechanism of indole derivatives as anti-cancer agents with their major target is explored in detail in this article.

METHODS

Recent advances and mechanism of indole derivatives as anti-cancer agents are reviewed. This review suggests a detailed explanation of multiple mechanisms of action of various indole derivatives: cell cycle arrest, aromatase inhibitor estrogen receptor regulator, tubulin inhibitor, a tyrosine kinase inhibitor, topoisomerase inhibitors, and NFkB/PI3/Akt/mTOR pathway inhibitors, through which these derivatives have shown promising anti-cancer potential.

RESULTS

A full literature review showed that the indole derivatives are associated with the properties of inducing apoptosis, aromatase inhibition, regulation of estrogen receptor and inhibition of tyrosine kinase, tubulin assembly, NFkB/PI3/Akt/mTOR pathway, and HDACs. These derivatives have shown significant activity against cancer cell lines.

CONCLUSION

Indole derivatives seem to be important in cancer via acting through various mechanisms. This review has shown that the indole derivatives can further be explored for the betterment of cancer treatment, and to discover the hidden potential of indole derivatives.

摘要

背景

癌症每年导致数人死亡。有多种经美国食品和药物管理局批准的癌症治疗药物。由于严重的副作用和多药耐药性,目前的药物疗法变得无效。因此,有必要开发具有较少毒性作用的新型药物。

目的

本文详细探讨了吲哚衍生物作为抗癌药物的作用机制及其主要靶点。

方法

综述了吲哚衍生物作为抗癌药物的最新进展和作用机制。这篇综述详细解释了各种吲哚衍生物的多种作用机制:细胞周期停滞、芳香酶抑制剂雌激素受体调节剂、微管抑制剂、酪氨酸激酶抑制剂、拓扑异构酶抑制剂和 NFkB/PI3/Akt/mTOR 通路抑制剂,这些衍生物通过这些机制显示出有希望的抗癌潜力。

结果

全面的文献回顾表明,吲哚衍生物与诱导细胞凋亡、芳香酶抑制、雌激素受体调节和抑制酪氨酸激酶、微管组装、NFkB/PI3/Akt/mTOR 通路和组蛋白去乙酰化酶的性质有关。这些衍生物对癌细胞系表现出显著的活性。

结论

吲哚衍生物似乎通过多种机制在癌症中起重要作用。本综述表明,吲哚衍生物可以进一步探索用于改善癌症治疗,并发现吲哚衍生物的潜在价值。

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