Ferrocenyl ferroptosis inducers as an emerging class of anticancer agents: a mini review

IF 3.597 Q2 Pharmacology, Toxicology and Pharmaceutics
MedChemComm Pub Date : 2025-12-29 DOI:10.1039/D5MD00935A
Mateusz Klarek, Aryan Gautam and Konrad Kowalski
{"title":"Ferrocenyl ferroptosis inducers as an emerging class of anticancer agents: a mini review","authors":"Mateusz Klarek, Aryan Gautam and Konrad Kowalski","doi":"10.1039/D5MD00935A","DOIUrl":null,"url":null,"abstract":"<p >Ferroptosis is one of the regulated cell death pathways. Molecular mechanisms underlying ferroptosis involve iron-dependent lipid peroxidation, which results in cell-deleterious membrane damage. Ferroptosis-inducing agents have been identified as attractive candidates for anticancer drug development as they can bypass drug resistance in cancer cells. Among pro-ferroptotic agents are many organometallic complexes, including ferrocenyl compounds. In this review, we demonstrate that suitably designed ferrocene-containing molecules can induce ferroptosis in different cancer cell types both <em>in vitro</em> and <em>in vivo</em>. Their pro-ferroptotic activity is triggered by diverse initiating factors through different mechanisms (<em>e.g.</em> redox activation, thermal and light activation, and GPX4 inhibition combined with ROS overproduction). Moreover, ferrocenyl bioconjugates are often cancer-cell-selective and trigger ferroptosis in combination with other regulated cell-death pathways, such as apoptosis and immunogenic cell death. Dual or multimodal anticancer activity mechanisms are sought after in modern anticancer therapy approaches as they help to overcome the problem of drug resistance. Research on ferrocene-based ferroptosis inducers, however, is still in the early stage. Hence, more time and effort are needed to fully elucidate the potential of ferrocenes as ferroptosis initiators in cancer therapy.</p>","PeriodicalId":88,"journal":{"name":"MedChemComm","volume":" 3","pages":" 1252-1270"},"PeriodicalIF":3.5970,"publicationDate":"2025-12-29","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"MedChemComm","FirstCategoryId":"1085","ListUrlMain":"https://pubs.rsc.org/en/content/articlelanding/2026/md/d5md00935a","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
引用次数: 0

Abstract

Ferroptosis is one of the regulated cell death pathways. Molecular mechanisms underlying ferroptosis involve iron-dependent lipid peroxidation, which results in cell-deleterious membrane damage. Ferroptosis-inducing agents have been identified as attractive candidates for anticancer drug development as they can bypass drug resistance in cancer cells. Among pro-ferroptotic agents are many organometallic complexes, including ferrocenyl compounds. In this review, we demonstrate that suitably designed ferrocene-containing molecules can induce ferroptosis in different cancer cell types both in vitro and in vivo. Their pro-ferroptotic activity is triggered by diverse initiating factors through different mechanisms (e.g. redox activation, thermal and light activation, and GPX4 inhibition combined with ROS overproduction). Moreover, ferrocenyl bioconjugates are often cancer-cell-selective and trigger ferroptosis in combination with other regulated cell-death pathways, such as apoptosis and immunogenic cell death. Dual or multimodal anticancer activity mechanisms are sought after in modern anticancer therapy approaches as they help to overcome the problem of drug resistance. Research on ferrocene-based ferroptosis inducers, however, is still in the early stage. Hence, more time and effort are needed to fully elucidate the potential of ferrocenes as ferroptosis initiators in cancer therapy.

Abstract Image

Abstract Image

二茂铁铁下垂诱导剂作为一类新兴的抗癌药物:综述。
铁下垂是受调控的细胞死亡途径之一。铁下垂的分子机制涉及铁依赖性脂质过氧化,导致细胞有害的膜损伤。诱导铁凋亡的药物已被确定为抗癌药物开发的有吸引力的候选者,因为它们可以绕过癌细胞的耐药性。在亲铁剂中有许多有机金属配合物,包括二茂铁基化合物。在这篇综述中,我们证明了适当设计的含二茂铁分子可以在体外和体内诱导不同类型的癌细胞铁凋亡。它们的亲铁性是由多种启动因子通过不同的机制触发的(如氧化还原激活、热和光激活、GPX4抑制结合ROS过量产生)。此外,二茂铁基生物偶联物通常具有癌细胞选择性,并与其他受调节的细胞死亡途径(如细胞凋亡和免疫原性细胞死亡)联合引发铁死亡。双重或多模态抗癌活性机制是现代抗癌治疗方法所追求的,因为它们有助于克服耐药性问题。然而,基于二茂铁的铁下垂诱导剂的研究仍处于早期阶段。因此,需要更多的时间和精力来充分阐明二茂铁作为铁下垂引发剂在癌症治疗中的潜力。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
求助全文
约1分钟内获得全文 求助全文
来源期刊
MedChemComm
MedChemComm BIOCHEMISTRY & MOLECULAR BIOLOGY-CHEMISTRY, MEDICINAL
CiteScore
4.70
自引率
0.00%
发文量
0
审稿时长
2.2 months
期刊介绍: Research and review articles in medicinal chemistry and related drug discovery science; the official journal of the European Federation for Medicinal Chemistry. In 2020, MedChemComm will change its name to RSC Medicinal Chemistry. Issue 12, 2019 will be the last issue as MedChemComm.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:604180095
Book学术官方微信
小红书