Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 9, Pages 2801-2805Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.03.061
Keywords
Pim-1 kinase; Inhibitors; Styrylquinolines; Quinoline-2-carboxamides; Molecular docking
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Funding
- Tishreen University, Lattakia, (Syria)
- Canceropole Grand-Ouest
- 'Association France-Alzheimer Finistere
- Association pour la Recherche sur le Cancer [ARC-1092]
- Ligue Nationale contre le Cancer
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Pim-1 kinase is a cytoplasmic serine/threonine kinase that controls programmed cell death by phosphorylating substrates that regulate both apotosis 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-hydroxyquinoline 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. (C) 2010 Elsevier Ltd. All rights reserved.
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