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Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors

  作者 Chioua, M; Samadi, A; Soriano, E; Lozach, O; Meijer, L; Marco-Contelles, J  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-16;  页码  4566-4569  
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[摘要]The synthesis and biological evaluation of a number of differently substituted 3,6-diamino-1H-pyrazolo[3,4-b] pyridine derivatives are reported. From the inhibition results on a selection of disease-relevant protein kinases [IC50 (mu M) DYRK1A = 11; CDK5 = 0.41; GSK-3 = 1.5] we have observed that 3,6-diamino-4-phenyl-1H-pyrazolo[3,4-b]pyridine-5-carbonitrile (4) constitutes a potential new and simple lead compound in the search of drugs for the treatment of Alzheimer's disease. (C) 2009 Elsevier Ltd. All rights reserved.

 
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