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A novel class of small molecule inhibitors with radioprotective properties
J. Marek, A. Tichy, R. Havelek, M. Seifrtova, A. Filipova, L. Andrejsova, T. Kucera, L. Prchal, L. Muckova, M. Rezacova, Z. Sinkorova, J. Pejchal,
European journal of medicinal chemistry.
2020 ;
187 (-) :
111606.
[pub] 20200101
Language English Country France
Document type Journal Article
Persistent link
https://www.medvik.cz/link/bmc20005591
- MeSH
- Apoptosis drug effects MeSH
- Small Molecule Libraries chemical synthesis chemistry pharmacology MeSH
- Humans MeSH
- Molecular Structure MeSH
- Mice, Inbred C57BL MeSH
- Mice MeSH
- Cell Line, Tumor MeSH
- Cell Proliferation drug effects MeSH
- Propanols chemical synthesis chemistry pharmacology MeSH
- Radiation-Protective Agents chemical synthesis chemistry pharmacology MeSH
- Molecular Docking Simulation MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Mice MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
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 60Co ionizing gamma radiation. Selected candidates underwent in vivo testing in C57Bl/6 J mice having a positive impact on their immunological status. In summary, we report here promising compounds with radioprotective effect in vivo.
References provided by Crossref.org
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