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

…, O Lozach, L Meijer, J Marco-Contelles

Index: Chioua, Mourad; Samadi, Abdelouahid; Soriano, Elena; Lozach, Olivier; Meijer, Laurent; Marco-Contelles, Jose Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 16 p. 4566 - 4569

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Citation Number: 48

Abstract

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 (μM) 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 ...