| Literature DB >> 15080992 |
Andrew J Peat1, Joyce A Boucheron, Scott H Dickerson, Dulce Garrido, Wendy Mills, Jennifer Peckham, Frank Preugschat, Terrence Smalley, Stephanie L Schweiker, Jayme R Wilson, Tony Y Wang, Huiqiang Q Zhou, Stephen A Thomson.
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 (Ar(1)) 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 GSK-3 inhibitors in the low nano-molar range.Entities:
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Year: 2004 PMID： 15080992 DOI： 10.1016/j.bmcl.2004.02.036
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823