Anticancer Activity of Spirocyclic Hydroxamic Acids (Derivatives of 1-Hydroxy-1,4,8-Triazaspiro[4,5]Decan-2-One), Histone Deacetylase Inhibitors
| Autor: | Natalia Akentieva, A. R. Gizatullin, N. I. Shkondina, I. V. Vystorop, T. A. Raevskaya, N. S. Goryachev, S. A. Goncharova, T. R. Prichodchenko, S. S. Shushanov |
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| Rok vydání: | 2019 |
| Předmět: |
0301 basic medicine
chemistry.chemical_classification Cisplatin Antitumor activity Chemistry Imidazolidinone education Biophysics Cell Biology Biochemistry 03 medical and health sciences chemistry.chemical_compound 030104 developmental biology 0302 clinical medicine Enzyme In vivo parasitic diseases medicine Piperidine Histone deacetylase Pharmacophore 030217 neurology & neurosurgery medicine.drug |
| Zdroj: | Biochemistry (Moscow), Supplement Series A: Membrane and Cell Biology. 13:12-23 |
| ISSN: | 1990-7494 1990-7478 |
| DOI: | 10.1134/s1990747818040037 |
| Popis: | The effect of 10 racemic spirocyclic hydroxamic acids (CHA 1–10, derivatives of 1-hydroxy-1,4,8-triazaspiro[4,5]decan-2-one), containing pharmacophore imidazolidinone and piperidine fragments with different substituents, on the activity of enzyme histone deacetylase (HDAC) was studied. It was shown that CHA (1–10) inhibit HDAC activity in cultured breast cancer cells. It was shown that CHA (1–10) as a part of polychemotherapy with cisplatin and cyclophosphane have a pronounced chemosensitizing antitumor activity in vivo. The results obtained on tumor models in vivo showed that CHA can be considered as potential medicinal components of tumor polychemotherapy. |
| Databáze: | OpenAIRE |
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