Synthesis and biological evaluation of 3,6-diamino-1H-pyrazolo[3,4-b]pyridine derivatives as protein kinase inhibitors |
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| Authors: | Mourad Chioua Abdelouahid Samadi Elena Soriano Olivier Lozach Laurent Meijer José Marco-Contelles |
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| Affiliation: | 1. Laboratorio de Radicales Libres y Química Computacional (IQOG, CSIC), 3, Juan de la Cierva, 28006 Madrid, Spain;2. Protein Phosphorylation and Human Disease Group, USR3151, Station Biologique, B.P. 74, 29682 Roscoff Cedex, Bretagne, France |
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| 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 drugs for the treatment of Alzheimer’s disease. |
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