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Substituted Piperazines as Novel Potential Radioprotective Agents
Molecules ( IF 4.2 ) Pub Date : 2020-01-25 , DOI: 10.3390/molecules25030532
Alzbeta Filipova 1 , Jan Marek 2 , Radim Havelek 3 , Jaroslav Pejchal 4 , Marcela Jelicova 1 , Jana Cizkova 1 , Martina Majorosova 3 , Lubica Muckova 4 , Tomas Kucera 4 , Lukas Prchal 2 , Miroslav Psotka 2 , Natalie Zivna 2 , Darja Koutova 3 , Zuzana Sinkorova 1 , Martina Rezacova 3 , Ales Tichy 1
Affiliation  

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.

中文翻译:

作为新型潜在辐射防护剂的取代哌嗪

辐射暴露风险的增加凸显了对新型辐射防护剂的需求。因此,设计并合成了一系列新型1-(2-羟乙基)哌嗪衍生物。一些化合物保护人体细胞免受辐射诱导的细胞凋亡,并表现出低细胞毒性。与之前的一系列哌嗪衍生物相比,化合物 8 在体外对细胞存活具有辐射防护作用,体内毒性较低。它还提高了全身照射后 30 天小鼠的存活率(尽管这种增加没有统计学意义)。总之,我们的体外和体内数据表明,我们的一些化合物作为潜在的辐射防护剂对于进一步研究很有价值。
更新日期:2020-01-25
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