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Substituted Piperazines as Novel Potential Radioprotective Agents

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 cytotoxic...

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Detalles Bibliográficos
Autores principales: Filipova, Alzbeta, Marek, Jan, Havelek, Radim, Pejchal, Jaroslav, Jelicova, Marcela, Cizkova, Jana, Majorosova, Martina, Muckova, Lubica, Kucera, Tomas, Prchal, Lukas, Psotka, Miroslav, Zivna, Natalie, Koutova, Darja, Sinkorova, Zuzana, Rezacova, Martina, Tichy, Ales
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7038073/
https://www.ncbi.nlm.nih.gov/pubmed/31991816
http://dx.doi.org/10.3390/molecules25030532
Descripción
Sumario: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.