Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform
| Autor: | Cynthia Barrett, Alexandra E. Gould, Janice Chin, Mable Brunson, John Ringeling, Christopher Tsu, R. Scott Rowland, Krista Wager, Kara Hoar, Juan Gutierrez, He Xu, Dylan England, Kris Garcia, Christopher Blackburn, Kenneth Gigstad |
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| Rok vydání: | 2014 |
| Předmět: |
Gene isoform
Hydroxamic acid Pyrazine Chemistry Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science HDAC6 Hydroxamic Acids Biochemistry Histone Deacetylase Inhibitors chemistry.chemical_compound Pyrazines Drug Discovery Protein Isoforms Molecular Medicine Histone deacetylase Selectivity Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 24:5450-5454 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2014.10.022 |
| Popis: | Acyl derivatives of 4-(aminomethyl)-N-hydroxybenzamide are potent sub-type selective HDAC6 inhibitors. Constrained heterocyclic analogs based on 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine show further enhanced HDAC6 selectivity and inhibitory activity in cells. Homology models suggest that the heterocyclic spacer can more effectively access the wider catalytic channel of HDAC6 compared to other HDAC sub-types. |
| Databáze: | OpenAIRE |
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