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Substituted Piperazines as Novel Potential Radioprotective Agents.

ABSTRACT: 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.

SUBMITTER: Filipova A

PROVIDER: S-EPMC7038073 | biostudies-literature | 2020 Jan

REPOSITORIES: biostudies-literature

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Substituted Piperazines as Novel Potential Radioprotective Agents.

Filipova Alzbeta A Marek Jan J Havelek Radim R Pejchal Jaroslav J Jelicova Marcela M Cizkova Jana J Majorosova Martina M Muckova Lubica L Kucera Tomas T Prchal Lukas L Psotka Miroslav M Zivna Natalie N Koutova Darja D Sinkorova Zuzana Z Rezacova Martina M Tichy Ales A

Molecules (Basel, Switzerland) 20200125 3

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 <b>8</b> exhibited a radioprotective effect on cell survival in vitro and low toxicity in vivo. It also enhanced the survival o ...[more]

PMID: 31991816

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