Synthesis and evaluation of smart drugs with integrated functions for identifying and treating oxidative microenvironments associated with cellular ferroptosis DOI Creative Commons
Yibo Zhang, Rui Cai, Yu‐Qiang Ding

и другие.

Smart Molecules, Год журнала: 2024, Номер unknown

Опубликована: Окт. 21, 2024

Abstract Ferroptosis is a novel form of cell death driven by oxidative damage, and implicated in various pathological conditions, including neurodegenerative diseases, retinal ischemia‐reperfusion injury organs. Inhibiting ferroptosis has shown great promise as therapeutic strategy for these underscoring the urgent need to develop effective inhibitors. Although Ferrostatin‐1 (Fer‐1) potent inhibitor, its susceptibility oxidation metabolic inactivation limits clinical utility. In this study, accumulation peroxides resulting damage cellular microenvironment during were utilized design prodrugs with reactive oxygen species‐responsive features. This approach led development series inhibitors that capable recognizing diseased areas, allowing targeted release improved stability. The compounds demonstrated significant inhibitory effects selectivity against RSL‐3‐induced HK‐2 cells, compound a1 exhibiting an EC50 15.4 ± 0.7 μM, outperforming Fer‐1. These effectively identify associated ferroptosis, enabling Fer‐1, which prevents lipid peroxide inhibits ferroptosis. holds treating diseases related offering intelligent approach.

Язык: Английский

Ferroptosis role in complexity of cell death: unrevealing mechanisms in Parkinson’s disease and therapeutic approaches DOI
Anupam Awasthi,

Kousik Maparu,

Shamsher Singh

и другие.

Inflammopharmacology, Год журнала: 2025, Номер unknown

Опубликована: Фев. 25, 2025

Язык: Английский

Процитировано

4

Advances in Ferroptosis Research: A Comprehensive Review of Mechanism Exploration, Drug Development, and Disease Treatment DOI Creative Commons
Haojie Wang, Yuanyuan Xie

Pharmaceuticals, Год журнала: 2025, Номер 18(3), С. 334 - 334

Опубликована: Фев. 26, 2025

In recent years, ferroptosis, as an emerging modality of programmed cell death, has captured significant attention within the scientific community. This comprehensive review meticulously canvasses pertinent literature past few spanning multiple facets. It delves into intricate mechanisms underpinning tracks evolution its inducers and inhibitors, dissects roles in a diverse array diseases, well resultant therapeutic implications. A profound exploration is conducted functional ferroptosis-related molecules, intracellular pathways, metabolic cascades, signaling transduction routes. Novel ferroptosis inhibitors are introduced detail, covering their design blueprints, synthetic methodologies, bioactivity profiles. Moreover, exhaustive account provided regarding involvement malignancies, neurodegenerative disorders, cardiovascular ailments, other pathologies. By highlighting pivotal status potential regimens various this aspires to furnish thorough reference framework for future investigations clinical translations domain.

Язык: Английский

Процитировано

1

Oxazole-Based Ferroptosis Inhibitors with Promising Properties to Treat Central Nervous System Diseases DOI Creative Commons
Camilla Scarpellini, Greta Klejborowska, Caroline Lanthier

и другие.

Journal of Medicinal Chemistry, Год журнала: 2025, Номер unknown

Опубликована: Фев. 6, 2025

Ferroptosis plays an important role in the occurrence and development of many diseases, including neurodegenerative diseases. Thus, ferroptosis inhibitors able to cross blood-brain barrier may have therapeutic potential. The best so far are lipophilic radical trapping antioxidants (RTAs) that block lipid peroxidation membranes. Several generations ferrostatins been synthesized, among which UAMC-3203 showed high potency animal models with improved properties compared ferrostatin-1. To further improve its pharmacokinetics properties, drug-likeness, permeability, we modified by decreasing size molecule reducing polarity replacing sulfonamide first amide groups subsequently isosteric oxazoles. Herein, present design, synthesis, biological evaluation a novel series oxazole RTAs potency, excellent oral bioavailability, concentrations brain tissue.

Язык: Английский

Процитировано

0

Identification of Imidazo[1,2-a]pyridine-3-amine as a Novel Drug-like Scaffold for Efficious Ferroptosis Inhibition in vivo DOI
Jilei Wang,

Xuejing Fan,

Xinyu Han

и другие.

European Journal of Medicinal Chemistry, Год журнала: 2025, Номер unknown, С. 117516 - 117516

Опубликована: Март 1, 2025

Язык: Английский

Процитировано

0

Targeting Ferroptosis in Parkinson’s Disease: Mechanisms and Emerging Therapeutic Strategies DOI Open Access

Minghao Zhou,

Keyang Xu, Jianxian Ge

и другие.

International Journal of Molecular Sciences, Год журнала: 2024, Номер 25(23), С. 13042 - 13042

Опубликована: Дек. 4, 2024

Parkinson's disease (PD) is a common neurodegenerative disorder characterized by the loss of dopaminergic neurons in substantia nigra and accumulation α-synuclein brain. Ferroptosis, recently identified form regulated cell death, critical PD pathogenesis due to its association with iron deposition, overproduction reactive oxygen species, iron-dependent lipid peroxidation impaired clearance. This death mechanism closely linked several pathogenic processes PD, including aggregation, oxidative stress, mitochondrial dysfunction, microglia-induced neuroinflammation, neuromelanin accumulation. Given significant role ferroptosis these mechanisms, there increasing interest targeting for treatment. Several drugs have shown potential alleviating symptoms inhibiting ferroptosis. review aims consolidate current knowledge on assess therapeutic anti-ferroptosis drugs, highlighting promising directions future research clinical applications.

Язык: Английский

Процитировано

3

Synthesis and biological evaluation of ferrostatin-based diamide derivatives as new ferroptosis inhibitors DOI
Leiying Zheng,

Nai-Yu Zhang,

Hui Zheng

и другие.

Bioorganic & Medicinal Chemistry Letters, Год журнала: 2024, Номер unknown, С. 129974 - 129974

Опубликована: Сен. 1, 2024

Язык: Английский

Процитировано

1

Synthesis and evaluation of smart drugs with integrated functions for identifying and treating oxidative microenvironments associated with cellular ferroptosis DOI Creative Commons
Yibo Zhang, Rui Cai, Yu‐Qiang Ding

и другие.

Smart Molecules, Год журнала: 2024, Номер unknown

Опубликована: Окт. 21, 2024

Abstract Ferroptosis is a novel form of cell death driven by oxidative damage, and implicated in various pathological conditions, including neurodegenerative diseases, retinal ischemia‐reperfusion injury organs. Inhibiting ferroptosis has shown great promise as therapeutic strategy for these underscoring the urgent need to develop effective inhibitors. Although Ferrostatin‐1 (Fer‐1) potent inhibitor, its susceptibility oxidation metabolic inactivation limits clinical utility. In this study, accumulation peroxides resulting damage cellular microenvironment during were utilized design prodrugs with reactive oxygen species‐responsive features. This approach led development series inhibitors that capable recognizing diseased areas, allowing targeted release improved stability. The compounds demonstrated significant inhibitory effects selectivity against RSL‐3‐induced HK‐2 cells, compound a1 exhibiting an EC50 15.4 ± 0.7 μM, outperforming Fer‐1. These effectively identify associated ferroptosis, enabling Fer‐1, which prevents lipid peroxide inhibits ferroptosis. holds treating diseases related offering intelligent approach.

Язык: Английский

Процитировано

0