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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...
Autores principales: | , , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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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. |
format | Online Article Text |
id | pubmed-7038073 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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