Aim and Objective: Some ferrocenyl derivatives are active in vitro and in vivo against cancer. Generally, ferrocenyl derivatives for cancer research have three key components: a ferrocene moiety, a conjugated linker that lowers the oxidation potential and some derivative (peptide, nucleobase and others) that can interact with biomolecules. Since the pyrimidine fragment can easily pass through the membrane into the cells and become involved in metabolism; it appears to be promising. Furthermore, this fragment is an electron-acceptor group, so a spacer can be excluded. Therefore, the synthesis of 6-ferrocenylpyrimidin-4(3H)-one derivatives and the study of their anticancer activity have scientific and practical interest. </P><P> Methods: The syntheses of 6-ferrocenylpyrimidin-4(3H)-one derivatives were performed by the condensation of ethyl 3-ferrocenyl-3-oxopropionate with thiourea or acetamidine or guanidine. The cytotoxicity of four 6- ferrocenylpyrimidin-4(3H)-one derivatives was evaluated by using the MTT assay in vitro against Human breast adenocarcinoma MCF-7 and normal human skin fibroblast HSF cells. The tested derivatives induced a concentration-dependent cytotoxic response in cell lines. </P><P> Results: A study of the cytotoxic activity of 6-ferrocenylpyrimidin-4(3H)-one derivatives by the MTT test has found that all compounds have a dose-dependent toxic effect on the lines of breast cancer cells (MCF-7) and normal human fibroblast cells (HSF). The most pronounced cytotoxic effect is exhibited by 2-methyl-6-ferrocenylpyrimidin- 4(3H)-one (MCF-7, IC50 17 ± 1 µM). Conclusion: The experimental results confirm the importance of investigation and design of ferrocenylpyrimidin- 4(3H)-one derivatives as anticancer agents. Compounds where the pyrimidine derivatives are directly linked to the ferrocene unit rather than via a spacer group also may be of interest for antiproliferative drug design.
The paper presents the results of preclinical studies of the allergenic properties of a new drug bisphenol-5, which has pronounced anti-radical activity. An experimental study of the antioxidant was carried out in doses of 2, 5, 20 mg/kg in guinea pigs and rabbits. It was shown that bisphenol-5 is not able to cause a general anaphylaxis reaction (anaphylactic shock). By the method of skin applications, the absence of allergenic effects of the drug in animals was found. During the formulation of conjunctival tests in experimental and control animals, signs of hypersensitivity, both immediate and delayed, were not observed with respect to the test drug. Changes in body temperature, pulse rate, and the number of respiratory movements as a result of clinical studies of the state of the animal organism after applying bisphenol-5 were also not recorded. Thus, the drug Besphenol-5 in the studied doses and under the selected experimental conditions does not have a negative effect on the body of laboratory animals and does not have allergenic properties.
The paper presents the results of research on the selection of biological agents with antagonism to microorganisms affecting raw materials of plant origin. The antagonists selected at the first stage showed significant changes in the antagonistic activity of various isolates when the temperature of the medium increased to 450C. There was no decrease in activity in isolate 20, so it is resistant to high temperature. Isolate No.21 had a significant increase in antagonistic activity, it is likely to be more resistant to high temperatures and some biochemical enzymatic processes are stimulated, leading to increased antagonistic properties. And in isolates 9, 16 and 23, on the contrary, it was lowered, possibly due to the fact that the increased temperature causes structural and biochemical changes in the cell of the microorganism. Similarly, isolated isolates No.9, 16, 23, 21, and 15 had high antagonistic activity against micromycetes that contaminate plant-based feed.
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