Design of n-substituted amino caproic hydroxamic acid histone deacetylase inhibitors reveal an essential role for cap atomic composition
| Autor: | Yves Collette, Jean M. Brunel, Thomas Prebet, Chanaz Salmi-Smail, Norbert Vey, Audrey Restouin |
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| Předmět: |
Aminocaproates
Pharmacology Cancer Research Hydroxamic acid biology Stereochemistry chemistry.chemical_element Antineoplastic Agents Hydroxamic Acids Oxygen Sulfur Enzyme assay Histone Deacetylase Inhibitors chemistry.chemical_compound Histone chemistry Biochemistry Acetylation Cell culture Cell Line Tumor biology.protein Humans Molecular Medicine Histone deacetylase Cell Proliferation |
| Zdroj: | Scopus-Elsevier |
| Popis: | A series of N-substituted amino caproic hydroxamic acid histone deacetylase inhibitors derivatives was designed in good-toexcellent yields and evaluated for their antiproliferative activity in a panel of human cancer cell lines, showing half maximum effective concentration varying from 700 nM to > 100 μM. Interestingly, the replacement of a furyl group by a thienyl one impacted very significantly the cap role on this antiproliferative activity and on histone acetylation induced by these drugs in cell-based but also in cell-free enzyme assays, suggesting an important role of the electronic density attached to the oxygen or sulfur atoms. |
| Databáze: | OpenAIRE |
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