Novel uracil-based 2-aminoanilide and 2-aminoanilide-like derivatives: histone deacetylase inhibition and in-cell activities
| Autor: | Andrea Perrone, Lucia Altucci, Dante Rotili, Angela Nebbioso, Silvio Massa, Sergio Valente, Antonello Mai, Maria Tardugno, Floriana De Bellis |
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| Přispěvatelé: | Mai, A, Perrone, A, Nebbioso, Angela, Rotili, D, Valente, S, Tardugno, M, Massa, S, DE BELLIS, F, Altucci, Lucia |
| Rok vydání: | 2008 |
| Předmět: |
aminoanilide
apoptosis chromatin remodelling cytodifferentiation histone deacetylase non-hydroxamate Cellular differentiation Clinical Biochemistry Pharmaceutical Science Biochemistry Histone Deacetylases Histones chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Humans Uracil Molecular Biology Amination U937 cell biology Molecular Structure Organic Chemistry Biological activity Acetylation Cell Differentiation U937 Cells Recombinant Proteins Benzamidines Histone Deacetylase Inhibitors chemistry Apoptosis Cell culture Enzyme inhibitor biology.protein Molecular Medicine Histone deacetylase Granulocytes |
| Zdroj: | Bioorganicmedicinal chemistry letters. 18(8) |
| ISSN: | 1464-3405 |
| Popis: | A novel series of non-hydroxamate HDAC inhibitors (HDACi) showing a uracil group at the left and a 2-aminoanilide/2-aminoanilide-like portion at the right head have been reported. In particular, the new compounds incorporating a 2-aminoanilide moiety behaved as class I-selective HDACi. Compound 8, the most potent and class I-selective, showed weak apoptosis (higher than MS-275) joined to cytodifferentiating activity on U937 cells. Surprisingly, the highest differentiation was observed with 13, through an effect that seems to be unrelated to HDAC inhibition. |
| Databáze: | OpenAIRE |
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