Further exploration of DVD-445 as a lead thioredoxin reductase (TrxR) inhibitor for cancer therapy: Optimization of potency and evaluation of anticancer potential.
ATP Binding Cassette Transporter, Subfamily B, Member 1
/ antagonists & inhibitors
Antineoplastic Agents
/ chemical synthesis
Cell Proliferation
/ drug effects
Cell Survival
/ drug effects
Cells, Cultured
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Enzyme Inhibitors
/ chemical synthesis
Humans
Molecular Structure
Oxidative Stress
/ drug effects
Recombinant Proteins
/ metabolism
Structure-Activity Relationship
Thioredoxin Reductase 1
/ antagonists & inhibitors
Cancer cell defense mechanism
Covalent inhibitor
Michael acceptors
Oxidative stress
P-gp inhibition
Thioredoxin reductase
Ugi four-component reaction
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:
01 Apr 2020
01 Apr 2020
Historique:
received:
04
01
2020
revised:
29
01
2020
accepted:
03
02
2020
pubmed:
23
2
2020
medline:
5
11
2020
entrez:
23
2
2020
Statut:
ppublish
Résumé
A series of analogs of the earlier reported lead compound DVD-445 (thioredoxin reductase inhibitor with anticancer activity) has been synthesized via a modified Ugi reaction and investigated. Seven most potent compounds (with IC
Identifiants
pubmed: 32087464
pii: S0223-5234(20)30086-6
doi: 10.1016/j.ejmech.2020.112119
pii:
doi:
Substances chimiques
ATP Binding Cassette Transporter, Subfamily B, Member 1
0
Antineoplastic Agents
0
Enzyme Inhibitors
0
Recombinant Proteins
0
TXNRD1 protein, human
EC 1.8.1.9
Thioredoxin Reductase 1
EC 1.8.1.9
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
112119Informations de copyright
Copyright © 2020 Elsevier Masson SAS. All rights reserved.