Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase
| Autor: | Laurent Meijer, Mélina Blairvacq, Faten Sliman, Didier Desmaële, Jordi Rodrigo, Emilie Durieu |
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| Rok vydání: | 2010 |
| Předmět: |
Stereochemistry
Clinical Biochemistry Pharmaceutical Science Antineoplastic Agents Mitogen-activated protein kinase kinase Biochemistry MAP2K7 Structure-Activity Relationship Proto-Oncogene Proteins c-pim-1 Drug Discovery Computer Simulation c-Raf Molecular Biology Protein Kinase Inhibitors Serine/threonine-specific protein kinase Binding Sites MAP kinase kinase kinase biology Chemistry Organic Chemistry Cyclin-dependent kinase 2 biology.protein Quinolines Molecular Medicine Cyclin-dependent kinase 9 Casein kinase 2 |
| Zdroj: | Bioorganicmedicinal chemistry letters. 20(9) |
| ISSN: | 1464-3405 |
| Popis: | Pim-1 kinase is a cytoplasmic serine/threonine kinase that controls programmed cell death by phosphorylating substrates that regulate both apoptosis and cellular metabolism. A series of 2-styrylquinolines and quinoline-2-carboxamides has been identified as potent inhibitors of the Pim-1 kinase. The 8-hydroxy-quinoline 7-carboxylic acid moiety appeared to be a crucial pharmacophore for activity. Molecular modeling indicated that interaction of this scaffold with Asp186 and Lys67 residues within the ATP-binding pocket might be responsible for the kinase inhibitory potency. |
| Databáze: | OpenAIRE |
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