A novel class of small molecule inhibitors with radioprotective properties.
Animals
Apoptosis
/ drug effects
Cell Line, Tumor
Cell Proliferation
/ drug effects
Dose-Response Relationship, Drug
Humans
Mice
Mice, Inbred C57BL
Molecular Docking Simulation
Molecular Structure
Propanols
/ chemical synthesis
Radiation-Protective Agents
/ chemical synthesis
Small Molecule Libraries
/ chemical synthesis
Structure-Activity Relationship
1-(2-hydroxyethyl)piperazine derivative
In vitro
Ionizing radiation
Mice
Radioprotection
Synthesis
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 Feb 2020
01 Feb 2020
Historique:
received:
27
06
2019
revised:
01
08
2019
accepted:
07
08
2019
pubmed:
7
1
2020
medline:
13
3
2020
entrez:
6
1
2020
Statut:
ppublish
Résumé
The goal of this study was to develop novel radioprotective agents targeting the intrinsic apoptotic pathway and thus decreasing the radiation-induced damage. For that purpose, we designed, synthesized and analyzed ten new compounds based on the 1-(4-(2-hydroxyethyl)piperazin-1-yl)-3-phenoxypropan-2-ol leading structure. The cytotoxicity of the newly synthesized substances was tested in vitro on cell lines derived from different progenitor cells by WST-1 proliferation assay. MTT test was utilized to assess half-maximal inhibitory concentrations and maximum tolerated concentrations of novel compounds in A-549 cells. Screening for radioprotective properties was performed using flow-cytometry in MOLT-4 cells exposed to
Identifiants
pubmed: 31901334
pii: S0223-5234(19)30740-8
doi: 10.1016/j.ejmech.2019.111606
pii:
doi:
Substances chimiques
Propanols
0
Radiation-Protective Agents
0
Small Molecule Libraries
0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
111606Informations de copyright
Copyright © 2019 Elsevier Masson SAS. All rights reserved.