Naphthyl ketones: a new class of Janus kinase 3 inhibitors
| Autor: | Neil Rankine, Andrea M. Bamford, Daniel S. James, Vanessa Torr, Brown George Robert, Jonathan Bowyer, Eric J. Culbert, Eric Tang |
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| Rok vydání: | 2000 |
| Předmět: |
Ketone
Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Enzyme-Linked Immunosorbent Assay Naphthalenes Biochemistry Chemical synthesis Aminoketone Mannich Bases Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Humans Structure–activity relationship Enzyme Inhibitors Molecular Biology chemistry.chemical_classification biology Janus kinase 3 Organic Chemistry Janus Kinase 3 Ketones Protein-Tyrosine Kinases chemistry Enzyme inhibitor biology.protein Molecular Medicine Indicators and Reagents Enone Tyrosine kinase |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 10:575-579 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(00)00051-2 |
| Popis: | Potent inhibition of Janus kinase 3 was found for a series of naphthyl(beta-aminoethyl)ketones (e.g. 7, pIC50 = 7.1+/-0.3). Further studies indicated that these compounds fragment in less than 1 h by retro-Michael reaction in the Jak3 in vitro ELISA assay procedure. The breakdown product of 7, 2-naphthylvinyl ketone (22, pIC50 = 6.8+/-0.3) showed very similar inhibitory activity to 7. Compounds 7 (in neutral buffer) and 22 will be useful pharmacological tools for the investigation of the Janus tyrosine kinase Jak3. |
| Databáze: | OpenAIRE |
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