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.
Highlights
Ionizing radiation (IR) was discovered in the 19th century; since its use has had a dramatic impact on medicine, space travel, research, and the energy industry
We focused on various modifications of the part of the molecule attached to the basic 1-(2-hydroxyethyl)piperazine moiety
Several promising radioprotective agents have been synthesized de novo
Summary
Ionizing radiation (IR) was discovered in the 19th century; since its use has had a dramatic impact on medicine, space travel, research, and the energy industry. Exposure to IR is associated with cell death, genetic mutations, and carcinogenesis [4]. DNA damage in the form of double-strand DNA breaks, which is considered the underlying mechanism of the resulting cell death: apoptosis. Apoptosis is a very complex process, which is tightly controlled in mammalian cells [5]. Its multi-level regulation has been the subject of medical research for a long time because some pathologies (such as cancer and autoimmune and neurodegenerative disease) are closely associated
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