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

被引：45
作者：
Sliman, Faten [1 ]
Blairvacq, Melina [2 ]
Durieu, Emilie [2 ]
Meijer, Laurent [2 ]
Rodrigo, Jordi [1 ]
Desmaele, Didier [1 ]
机构：
[1] Univ Paris Sud, UMR BIOCIS 89076, Fac Pharm, F-92296 Chatenay Malabry, France
[2] Biol Stn, USR3151, Prot Phosphorylat & Human Dis Grp, F-29682 Roscoff, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 09期
关键词：
Pim-1; kinase; Inhibitors; Styrylquinolines; Quinoline-2-carboxamides; Molecular docking; HIV-1 REPLICATION INHIBITORS; PROSTATE-CANCER; BINDING MODE; BIOLOGICAL-ACTIVITIES; POTENT; PROTOONCOGENE; INTEGRASE; CELLS; STYRYLQUINOLINES; SPECIFICITY;
D O I：
10.1016/j.bmcl.2010.03.061
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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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收藏
页码：2801 / 2805
页数：5
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