Title of article
Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors
Author/Authors
Andrew J. Peat، نويسنده , , Joyce A Boucheron، نويسنده , , Scott H Dickerson، نويسنده , , Dulce Garrido، نويسنده , , Wendy Mills، نويسنده , , Jennifer Peckham، نويسنده , , Frank Preugschat، نويسنده , , Terrence Smalley، نويسنده , , Stephanie L Schweiker، نويسنده , , Jayme L.R. Wilson، نويسنده , , Tony Y Wang، نويسنده , , Huiqiang Q Zhou، نويسنده , , Stephen A Thomson، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
2121
To page
2125
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 GSK-3 inhibitors in the low nano-molar range.
Keywords
Glycogen synthase kinase-3.* Correspondingauthor. Tel.: +1-919-483-6287 , fax: +1-919-483-6053 , e-mail: stephen.a.thomson@gsk.com
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794351
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