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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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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
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author 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
author_facet 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
author_sort Filipova, Alzbeta
collection PubMed
description 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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spelling pubmed-70380732020-03-10 Substituted Piperazines as Novel Potential Radioprotective Agents 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 Molecules Article 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. MDPI 2020-01-25 /pmc/articles/PMC7038073/ /pubmed/31991816 http://dx.doi.org/10.3390/molecules25030532 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
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
Substituted Piperazines as Novel Potential Radioprotective Agents
title Substituted Piperazines as Novel Potential Radioprotective Agents
title_full Substituted Piperazines as Novel Potential Radioprotective Agents
title_fullStr Substituted Piperazines as Novel Potential Radioprotective Agents
title_full_unstemmed Substituted Piperazines as Novel Potential Radioprotective Agents
title_short Substituted Piperazines as Novel Potential Radioprotective Agents
title_sort substituted piperazines as novel potential radioprotective agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7038073/
https://www.ncbi.nlm.nih.gov/pubmed/31991816
http://dx.doi.org/10.3390/molecules25030532
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