A novel class of small molecule inhibitors with radioprotective properties
Jazyk angličtina Země Francie Médium print-electronic
Typ dokumentu časopisecké články
PubMed
31901334
DOI
10.1016/j.ejmech.2019.111606
PII: S0223-5234(19)30740-8
Knihovny.cz E-zdroje
- Klíčová slova
- 1-(2-hydroxyethyl)piperazine derivative, In vitro, Ionizing radiation, Mice, Radioprotection, Synthesis,
- MeSH
- apoptóza účinky léků MeSH
- knihovny malých molekul chemická syntéza chemie farmakologie MeSH
- lidé MeSH
- molekulární struktura MeSH
- myši inbrední C57BL MeSH
- myši MeSH
- nádorové buněčné linie MeSH
- proliferace buněk účinky léků MeSH
- propanoly chemická syntéza chemie farmakologie MeSH
- radioprotektivní látky chemická syntéza chemie farmakologie MeSH
- simulace molekulového dockingu MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- myši MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- knihovny malých molekul MeSH
- propanoly MeSH
- radioprotektivní látky 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.
Citace poskytuje Crossref.org
Second-generation piperazine derivatives as promising radiation countermeasures
Substituted Piperazines as Novel Potential Radioprotective Agents
