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Novel 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitrile derivatives as dual cyclin-dependent kinase 1 (CDK1)/glycogen synthase kinase-3 (GSK-3) inhibitors: Synthesis, biological evaluation and molecular modeling studies

  作者 Logee, C; Testard, A; Thieery, V; Lozach, O; Blairvacq, M; Robert, JM; Meijer, L; Besson, T  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2008年43-7;  页码  1469-1477  
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[摘要]

Continuous efforts in microwave-assisted synthesis and the structure-activity relationships' (SARs) studies of novel modified 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitriles, allowed identification of new amidine and imidate derivatives as potent and dual CDK1/GSK-3 inhibitors. Combination of lead optimization and molecular modeling studies allowed identification of a dual CDK1/GSK-3 inhibitor (compound 13d) with submicromolar values. (c) 2007 Elsevier Masson SAS. All rights reserved.

 
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