Discovery of 4-hydroxyl pyrazole derivatives as potent ferroptosis inhibitors.

Ferroptosis Antioxidants / pharmacology Cell Line Iron / metabolism Hydroxyl Radical Hydrocarbons Pyrazoles / pharmacology
4-Hydroxyl pyrazole derivatives Ferroptosis inhibitor Radical-trapping antioxidant Structure-activity relationship

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
05 Jan 2024
Historique:
received: 04 09 2023
revised: 11 10 2023
accepted: 24 10 2023
medline: 4 12 2023
pubmed: 12 11 2023
entrez: 11 11 2023
Statut: ppublish

Résumé

Ferroptosis, an iron-dependent form of regulated cell death, has been well recognized as a pathogenic mechanism in driving many diseases, such as neurodegenerative disorders, ischemia-reperfusion (I/R) injury. Blocking ferroptosis has been emerging as a feasible therapeutic strategy for the prevention and treatment of these diseases. However, novel potent ferroptosis inhibitors remain to be developed for further clinical applications. In this study, we screened our in-house compound libraries by phenotypic assays and identified a 4-hydroxyl pyrazole derivative HW-3 with good ferroptosis inhibitory activity (EC

Identifiants

DOI: 10.1016/j.ejmech.2023.115913 PMID: 37950965
pubmed: 37950965
pii: S0223-5234(23)00880-2
doi: 10.1016/j.ejmech.2023.115913
pii:
doi:

Substances chimiques

Antioxidants 0
Iron E1UOL152H7
Hydroxyl Radical 3352-57-6
Hydrocarbons 0
Pyrazoles 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

115913

Informations de copyright

Copyright © 2023. Published by Elsevier Masson SAS.

Déclaration de conflit d'intérêts

Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Danzhi Ying (D)

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.

Xin Shen (X)

The First Affiliated Hospital, The Second Affiliated Hospital, Institute of Translational Medicine, School of Public Health, Zhejiang University School of Medicine, Hangzhou, 310058, China.

Shuqi Wang (S)

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.

Junyi Chen (J)

The First Affiliated Hospital, The Second Affiliated Hospital, Institute of Translational Medicine, School of Public Health, Zhejiang University School of Medicine, Hangzhou, 310058, China.

Zhenying Wu (Z)

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.

Wenteng Chen (W)

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China.

Fudi Wang (F)

The First Affiliated Hospital, The Second Affiliated Hospital, Institute of Translational Medicine, School of Public Health, Zhejiang University School of Medicine, Hangzhou, 310058, China.

Junxia Min (J)

The First Affiliated Hospital, The Second Affiliated Hospital, Institute of Translational Medicine, School of Public Health, Zhejiang University School of Medicine, Hangzhou, 310058, China. Electronic address: junxiamin@zju.edu.cn.

Yongping Yu (Y)

College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 310058, China. Electronic address: yyu@zju.edu.cn.

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Classifications MeSH

questionsmedicales.fr › Phénomènes physiologiques cellulaires › Mort cellulaire › Mort cellulaire régulée › Ferroptose › Discovery of 4-hydroxyl pyrazole derivatives...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Agents protecteurs › Antioxydants › Discovery of 4-hydroxyl pyrazole derivatives...
questionsmedicales.fr › Cellules › Cellules cultivées › Lignée cellulaire › Discovery of 4-hydroxyl pyrazole derivatives...
questionsmedicales.fr › Produits chimiques inorganiques › Métaux › Métaux lourds › Fer › Discovery of 4-hydroxyl pyrazole derivatives...
questionsmedicales.fr › Produits chimiques inorganiques › Radical hydroxyle › Discovery of 4-hydroxyl pyrazole derivatives...
questionsmedicales.fr › Composés chimiques organiques › Hydrocarbures › Discovery of 4-hydroxyl pyrazole derivatives...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Pyrazoles › Discovery of 4-hydroxyl pyrazole derivatives...