864871-85-2Relevant articles and documents
Identification of novel GLUT inhibitors
Siebeneicher, Holger,Bauser, Marcus,Buchmann, Bernd,Heisler, Iring,Müller, Thomas,Neuhaus, Roland,Rehwinkel, Hartmut,Telser, Joachim,Zorn, Ludwig
, p. 1732 - 1737 (2016/07/27)
The compound class of 1H-pyrazolo[3,4-d]pyrimidines was identified using HTS as very potent inhibitors of facilitated glucose transporter 1 (GLUT1). Extensive structure–activity relationship studies (SAR) of each ring system of the molecular framework was established revealing essential structural motives (i.e., ortho-methoxy substituted benzene, piperazine and pyrimidine). The selectivity against GLUT2 was excellent and initial in vitro and in vivo pharmacokinetic (PK) studies are encouraging.
Novel pyrazolopyrimidine derivatives as GSK-3 inhibitors
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.
, p. 2121 - 2125 (2007/10/03)
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.
