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“Double” Pyrimidine Derivatives: Synthesis and Primary Assessment of Hepatoprotective Properties In Vitro

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Abstract

“Double” derivatives of the drug Xymedon (1,2-dihydro-4,6-dimethyl-1-N-(hydroxyethyl)pyrimidone-2), hereafter referred to as pyrimidine (I), in which the pyrimidine (I) molecules are joined by an alkyl(xylylenyl)dionate bridge have been synthesized. Primary data on the hepatoprotective activity of five “double” pyrimidine (I) derivatives with different numbers of methylene groups and a meta-xylylene fragment in the ester bridge have been obtained on normal human hepatocytes of the Chang Liver cell line. The cytotoxicity and the cytoprotective properties of the new compounds against the background of exposure to d-galactosamine at a concentration of 150 mmol/L have been determined, their effect on the cell cycle compared with that of the initial pyrimidine (I) has been studied, and the dependence of the biological properties of the derivatives on their structure has been established.

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ACKNOWLEDGMENTS

The authors would like to thank the Collective Spectral-Analytical Center of Physicochemical Investigations, Kazan Research Center, Russian Academy of Sciences, for technical assistance in conducting the study.

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Authors and Affiliations

  1. Arbuzov Institute of Organic and Physical Chemistry, Kazan Research Center, Russian Academy of Sciences, 420088, Kazan, Russia

    A. B. Vyshtakalyuk, V. E. Semenov, A. A. Parfenov, M. S. Shashyn, G. P. Belyaev, I. V. Galyametdinova & V. V. Zobov

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  1. A. B. Vyshtakalyuk
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  2. V. E. Semenov
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  3. A. A. Parfenov
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  4. M. S. Shashyn
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  5. G. P. Belyaev
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  6. I. V. Galyametdinova
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  7. V. V. Zobov
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Corresponding author

Correspondence to A. B. Vyshtakalyuk.

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The paper does not contain any studies involving animal or human participants performed by any of the authors.

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The authors declare that there is no conflict of interest.

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Translated by S. Sidorova

Abbreviations: d-GLA, d-galactosamine; IC50, the concentration of a substance that causes the death of 50% of cells; cell cycle phases: G0/G1, resting/presynaptic phase; S, synthesis phase; G2/M, postsynthetic/mitotic phase.

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Vyshtakalyuk, A.B., Semenov, V.E., Parfenov, A.A. et al. “Double” Pyrimidine Derivatives: Synthesis and Primary Assessment of Hepatoprotective Properties In Vitro. Russ J Bioorg Chem 46, 1067–1073 (2020). https://doi.org/10.1134/S1068162020060369

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  • DOI: https://doi.org/10.1134/S1068162020060369

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