Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors

…, D Garrido, W Mills, J Peckham, F Preugschat…

Index: Peat, Andrew J.; Boucheron, Joyce A.; Dickerson, Scott H.; Garrido, Dulce; Mills, Wendy; Peckham, Jennifer; Preugschat, Frank; Smalley, Terrence; Schweiker, Stephanie L.; Wilson, Jayme R.; Wang, Tony Y.; Zhou, Huiqiang Q.; Thomson, Stephen A. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 9 p. 2121 - 2125

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Citation Number: 62

Abstract

A series of [1-aryl-1H-pyrazolo [3, 4-d] pyrimidin-4-yl] arylhydrazones were discovered as novel inhibitors glycogen synthase kinase-3 (GSK-3). Based on initial modeling a detailed SAR was constructed. Modification of the interior binding aryl ring (Ar1) determined this to be a tight binding region with little room for modification. As predicted from the model, a large variety of modifications could be incorporated into the hydrazone aryl ring. This work led to ...

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