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Substituted Piperazines as Novel Potential Radioprotective Agents
A. Filipova, J. Marek, R. Havelek, J. Pejchal, M. Jelicova, J. Cizkova, M. Majorosova, L. Muckova, T. Kucera, L. Prchal, M. Psotka, N. Zivna, D. Koutova, Z. Sinkorova, M. Rezacova, A. Tichy,
Language English Country Switzerland
Document type Journal Article
Grant support
17-13541S
Grantová Agentura České Republiky
NLK
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from 1997-01-01
- MeSH
- Survival Analysis MeSH
- Radiation, Ionizing MeSH
- Humans MeSH
- Maximum Tolerated Dose MeSH
- Molecular Conformation MeSH
- Models, Molecular MeSH
- Molecular Structure MeSH
- Cell Line, Tumor MeSH
- Piperazines administration & dosage adverse effects chemistry pharmacology MeSH
- Radiation-Protective Agents administration & dosage adverse effects chemistry pharmacology MeSH
- Cell Survival drug effects radiation effects MeSH
- Dose-Response Relationship, Drug MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
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.
References provided by Crossref.org
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- $a 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.
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