Cytotoxic and Antiviral Properties of Novel Dehydroabietylamine Salts

Kovaleva, Kseniya S.; Kononova, A. A.; Korobeynikov, Vladislav A.; Чересиз, С. В.; Zarubaev, Vladimir V.; Штро, Анна А.; Orshanskaya, Yana R.; Yarovaya, Оlga I.; Pokrovsky, Andrey G.; Салахутдинов, Н. Ф.

doi:10.4172/2161-0444.1000408

Cited by 5 publications

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“…Since dehydroabietylamine and its derivatives are known to possess high cytotoxicity against several cancer cells lines [ 36 , 37 , 38 ], the ureas, thioureas, amides, and thioamide ( 1 – 12 ) synthesised in the present study were tested against the T98G glioma cells. Since we used the T98G glioblastoma cell line for the first time for our experiments, we first attempted to perform the cytotoxicity study in a range of concentrations from 10 to 100 µM, as we did previously with the TDP1 inhibitory compounds when working with the other cell lines.…”

Section: Resultsmentioning

confidence: 99%

Design, Synthesis, and Molecular Docking Study of New Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors Combining Resin Acids and Adamantane Moieties

et al. 2021

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In this paper, a series of novel abietyl and dehydroabietyl ureas, thioureas, amides, and thioamides bearing adamantane moieties were designed, synthesized, and evaluated for their inhibitory activities against tyrosil-DNA-phosphodiesterase 1 (TDP1). The synthesized compounds were able to inhibit TDP1 at micromolar concentrations (0.19–2.3 µM) and demonstrated low cytotoxicity in the T98G glioma cell line. The effect of the terpene fragment, the linker structure, and the adamantane residue on the biological properties of the new compounds was investigated. Based on molecular docking results, we suppose that adamantane derivatives of resin acids bind to the TDP1 covalent intermediate, forming a hydrogen bond with Ser463 and hydrophobic contacts with the Phe259 and Trp590 residues and the oligonucleotide fragment of the substrate.

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Section: Resultsmentioning

confidence: 99%

Design, Synthesis, and Molecular Docking Study of New Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors Combining Resin Acids and Adamantane Moieties

et al. 2021

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“…In [29], a study of the antiviral activity of dehydroabiethylamine salts with modified organic acids against the influenza A/California/07/09 (H1N1) pdm09 strain was carried out. It was shown that the modification of dehydroabiethylamine with counterions of organic acids did not lead to an increase in antiviral activity.…”

Section: Discussionmentioning

confidence: 99%

Rosin Derivatives as a Platform for the Antiviral Drug Design

et al. 2021

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The increased complexity due to the emergence and rapid spread of new viral infections prompts researchers to search for potential antiviral and protective agents for mucous membranes among various natural objects, for example, plant raw materials, their individual components, as well as the products of their chemical modification. Due to their structure, resin acids are valuable raw materials of natural origin to synthesize various bioactive substances. Therefore, the purpose of this study was to confirm the possibility of using resin acid derivatives for the drug design. As a result, we studied the cytotoxicity and biological activity of resin acid derivatives. It was shown that a slight decrease in the viral load in the supernatants was observed upon stimulation of cells (II) compared with the control. When using PASS-online modeling (Prediction of Activity Spectra for Substances), the prediction of the biological activity spectrum showed that compound (I) is capable of exhibiting antiviral activity against the influenza virus. The use of the SWISS-ADME webserver to reveal the drug-like properties of compounds did not directly indicate the presence of antiviral activity. These results indicate the potential of resin acid derivatives as a starting point for extensive research in the study of biological activity.

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Syntheses and high selective cytotoxicity of dehydroabietylamine C-ring nitration derivatives

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Xue³

et al. 2022

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Cytotoxic and Antiviral Properties of Novel Dehydroabietylamine Salts

Cited by 5 publications

References 0 publications

Design, Synthesis, and Molecular Docking Study of New Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors Combining Resin Acids and Adamantane Moieties

Design, Synthesis, and Molecular Docking Study of New Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors Combining Resin Acids and Adamantane Moieties

Rosin Derivatives as a Platform for the Antiviral Drug Design

Syntheses and high selective cytotoxicity of dehydroabietylamine C-ring nitration derivatives

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