Minor structural modifications to Pracinostat produce big changes in its biological responses
| Autor: | Youjin Ge, Pengju Sun, Yan Zhang, Rong Jia, Niefang Yu |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Pharmacology
Benzimidazole Stereochemistry Pracinostat Organic Chemistry Histone Deacetylase 6 Biochemistry Histone Deacetylase Inhibitors chemistry.chemical_compound chemistry mental disorders Drug Discovery HDAC inhibitor Molecular Medicine Humans Benzimidazoles psychological phenomena and processes Derivative (chemistry) HeLa Cells |
| Zdroj: | Chemical biologydrug design. 94(2) |
| ISSN: | 1747-0285 |
| Popis: | A series of compounds similar to Pracinostat that contained benzimidazole ring and N-hydroxyacrylamide attached at 5- or 6-position were designed, synthesized, and evaluated as HDAC inhibitors. It was interesting to find that the corresponding derivative 1 with N-hydroxyacrylamide attached at 5-position was a potent HDAC inhibitor while the others at 6-position were not. This is the first time to demonstrate the position difference plays important role in the HDAC inhibitory activities of the cinnamic hydroxamates. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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