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Synthesis, docking study and kinase inhibitory activity of a number of new substituted pyrazolo[3,4-c]pyridines

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Sklepari, Meropi | Lougiakis, Nikolaos | Papastathopoulos, Athanasios | Pouli, Nicole | Marakos, Panagiotis | Myrianthopoulos, Vassilios | Robert, Thomas | Bach, Stéphane | Mikros, Emmanuel | Ruchaud, Sandrine

Edité par CCSD ; Pharmaceutical Society of Japan -

International audience. A series of new pyrazolo[3,4-c]pyridines bearing various 1, 3, 5 or 1, 3, 7 pattern substitutions, were designed and synthesized. Some of them showed interesting inhibitory activity mainly against GSK3α/β as well as against CLK1 and DYRK1A, with good selectivity and remarkable SARs, without being cytotoxic. Molecular simulations in corelation with biological data revealed the importance of the existence of N1-H as well as the absence of a bulky 7-substituent.

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