Substituted Piperazines as Novel Potential Radioprotective Agents.
Alzbeta FilipovaJan MarekRadim HavelekJaroslav PejchalMarcela JelicovaJana CizkovaMartina MajorosovaLubica MúčkováTomas KuceraLukas PrchalMiroslav PsotkaNatalie ZivnaDarja KoutovaZuzana SinkorovaMartina ŘezáčováJakub GreplPublished in: Molecules (Basel, Switzerland) (2020)
The increasing risk of radiation exposure underlines the need for novel radioprotective agents. Hence, a series of novel 1-(2-hydroxyethyl)piperazine derivatives were designed and synthesized. Some of the compounds protected human cells against radiation-induced apoptosis and exhibited low cytotoxicity. Compared to the previous series of piperazine derivatives, compound 8 exhibited a radioprotective effect on cell survival in vitro and low toxicity in vivo. It also enhanced the survival of mice 30 days after whole-body irradiation (although this increase was not statistically significant). Taken together, our in vitro and in vivo data indicate that some of our compounds are valuable for further research as potential radioprotectors.
Keyphrases
- induced apoptosis
- endoplasmic reticulum stress
- oxidative stress
- signaling pathway
- human health
- molecular docking
- electronic health record
- type diabetes
- structure activity relationship
- high fat diet induced
- metabolic syndrome
- radiation induced
- machine learning
- risk assessment
- adipose tissue
- skeletal muscle
- deep learning
- climate change