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芳基哌嗪衍生物与癌症:药物化学中的新挑战

Arylpiperazine Derivatives and Cancer: A New Challenge in Medicinal Chemistry.

作者信息

Andreozzi Giorgia, Corvino Angela, Severino Beatrice, Magli Elisa, Perissutti Elisa, Frecentese Francesco, Santagada Vincenzo, Caliendo Giuseppe, Fiorino Ferdinando

机构信息

Dipartimento di Farmacia, Università di Napoli Federico II, Via D. Montesano 49, 80131 Naples, Italy.

Dipartimento di Sanità Pubblica, Università di Napoli Federico II, Via Pansini 5, 80131 Naples, Italy.

出版信息

Pharmaceuticals (Basel). 2024 Oct 2;17(10):1320. doi: 10.3390/ph17101320.

Abstract

In recent decades, there has been a startling rise in the number of cancer patients worldwide, which has led to an amazing upsurge in the development of novel anticancer treatment candidates. On a positive note, arylpiperazines have garnered attention in cancer research due to their potential as scaffolds for developing anticancer agents. These compounds exhibit a diverse array of biological activities, including cytotoxic effects against cancer cells. Indeed, one of the key advantages of arylpiperazines lies in their ability to interact with various molecular targets implicated in cancer pathogenesis. Here, we focus on the chemical structures of several arylpiperazine derivatives, highlighting their anti-proliferative activity in different tumor cell lines. The modular structure, diverse biological activities, and potential for combination therapies of arylpiperazine compounds make them valuable candidates for further preclinical and clinical investigations in the fight against cancer. This review, providing a careful analysis of different arylpiperazines and their biological applications, allows researchers to refine the chemical structures to improve potency, selectivity, and pharmacokinetic properties, thus advancing their therapeutic potential in oncology.

摘要

近几十年来,全球癌症患者数量惊人地上升,这导致新型抗癌治疗候选药物的研发出现了惊人的热潮。积极的一面是,芳基哌嗪因其作为开发抗癌药物支架的潜力而在癌症研究中受到关注。这些化合物表现出多种生物活性,包括对癌细胞的细胞毒性作用。事实上,芳基哌嗪的一个关键优势在于它们能够与癌症发病机制中涉及的各种分子靶点相互作用。在此,我们聚焦于几种芳基哌嗪衍生物的化学结构,突出它们在不同肿瘤细胞系中的抗增殖活性。芳基哌嗪化合物的模块化结构、多样的生物活性以及联合治疗的潜力,使其成为进一步开展抗癌临床前和临床研究的有价值候选药物。这篇综述对不同的芳基哌嗪及其生物学应用进行了仔细分析,使研究人员能够优化化学结构以提高效力、选择性和药代动力学性质,从而提升它们在肿瘤学中的治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/72d4/11510360/e18da3877a39/pharmaceuticals-17-01320-g001.jpg

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