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Bioorg Med Chem Lett. 2010 May 1;20(9):2801-5. doi: 10.1016/j.bmcl.2010.03.061. Epub 2010 Mar 15.

Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.

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UMR 89076 BIOCIS, Faculté de Pharmacie, Université Paris Sud, 5 rue J.-B. Clément, 92296 Châtenay-Malabry, France.


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.

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