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咪唑类化合物作为潜在的抗癌剂:近期研究进展综述。

Imidazoles as Potential Anticancer Agents: An Update on Recent Studies.

机构信息

Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA.

Division of Mathematics, Computer & Natural Sciences Division, Ohio Dominican University, Columbus, OH 43219, USA.

出版信息

Molecules. 2021 Jul 11;26(14):4213. doi: 10.3390/molecules26144213.

Abstract

Nitrogen-containing heterocyclic rings are common structural components of marketed drugs. Among these heterocycles, imidazole/fused imidazole rings are present in a wide range of bioactive compounds. The unique properties of such structures, including high polarity and the ability to participate in hydrogen bonding and coordination chemistry, allow them to interact with a wide range of biomolecules, and imidazole-/fused imidazole-containing compounds are reported to have a broad spectrum of biological activities. This review summarizes recent reports of imidazole/fused imidazole derivatives as anticancer agents appearing in the peer-reviewed literature from 2018 through 2020. Such molecules have been shown to modulate various targets, including microtubules, tyrosine and serine-threonine kinases, histone deacetylases, p53-Murine Double Minute 2 (MDM2) protein, poly (ADP-ribose) polymerase (PARP), G-quadraplexes, and other targets. Imidazole-containing compounds that display anticancer activity by unknown/undefined mechanisms are also described, as well as key features of structure-activity relationships. This review is intended to provide an overview of recent advances in imidazole-based anticancer drug discovery and development, as well as inspire the design and synthesis of new anticancer molecules.

摘要

含氮杂环是市售药物中常见的结构组成部分。在这些杂环中,咪唑/稠合咪唑环存在于广泛的生物活性化合物中。这些结构的独特性质,包括高极性以及参与氢键和配位化学的能力,使它们能够与广泛的生物分子相互作用,并且据报道,含有咪唑/稠合咪唑的化合物具有广泛的生物活性。本文综述了 2018 年至 2020 年期间在同行评议文献中报道的作为抗癌剂的咪唑/稠合咪唑衍生物的最新研究进展。这些分子已被证明能够调节各种靶标,包括微管、酪氨酸和丝氨酸/苏氨酸激酶、组蛋白去乙酰化酶、p53-Murine Double Minute 2 (MDM2) 蛋白、多聚(ADP-核糖)聚合酶 (PARP)、G-四链体和其他靶标。本文还描述了通过未知/未定义机制显示抗癌活性的含咪唑化合物,以及结构-活性关系的关键特征。本文旨在提供基于咪唑的抗癌药物发现和开发的最新进展概述,并激发新的抗癌分子的设计和合成。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e082/8307698/74f0e545122b/molecules-26-04213-g001.jpg

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