Design, synthesis and biological evaluation of imidazolidine-2,4-dione and 2-thioxothiazolidin-4-one derivatives as lymphoid-specific tyrosine phosphatase inhibitors.
Cells, Cultured
Dose-Response Relationship, Drug
Drug Design
Enzyme Inhibitors
/ chemical synthesis
Humans
Imidazolidines
/ chemical synthesis
Jurkat Cells
Molecular Docking Simulation
Molecular Structure
Protein Tyrosine Phosphatase, Non-Receptor Type 22
/ antagonists & inhibitors
Structure-Activity Relationship
Thiazolidines
/ chemical synthesis
Autoimmune diseases
Inhibitor
Lymphoid-specific tyrosine phosphatase
Journal
Bioorganic chemistry
ISSN: 1090-2120
Titre abrégé: Bioorg Chem
Pays: United States
ID NLM: 1303703
Informations de publication
Date de publication:
10 2020
10 2020
Historique:
received:
25
12
2019
revised:
09
07
2020
accepted:
20
07
2020
pubmed:
10
8
2020
medline:
3
3
2021
entrez:
10
8
2020
Statut:
ppublish
Résumé
Lymphoid-specific tyrosine phosphatase (LYP), which exclusively exists in immune cells and down-regulates T cell receptor signaling (TCR), has becoming a potent target for various autoimmune diseases. Herein, we designed and synthesized imidazolidine-2,4-dione and 2-thioxothiazolidin-4-one derivatives as new LYP inhibitors. Among them, the cinnamic acids-based inhibitors (9p and 9r) displayed good LYP inhibitory activities (IC
Identifiants
pubmed: 32768742
pii: S0045-2068(20)31421-8
doi: 10.1016/j.bioorg.2020.104124
pii:
doi:
Substances chimiques
Enzyme Inhibitors
0
Imidazolidines
0
Thiazolidines
0
imidazolidine-2,4-dione
0
Protein Tyrosine Phosphatase, Non-Receptor Type 22
EC 3.1.3.48
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
104124Informations de copyright
Copyright © 2020 Elsevier Inc. All rights reserved.
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.