650628-11-8Relevant academic research and scientific papers
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 PYRAZOLO [3, 4 -D] PYRIMIDINE DERIVATIVES AS ANTI-CANCER AGENTS
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Page/Page column 37, (2010/12/29)
The invention relates to substituted pyrazolo[3,4-d]pyrimidine derivatives of the Formula-(I), or pharmaceutically acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted pyrazolo[3,4-d]pyrimidine derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti-proliferative effect in a warm-blooded animal such as man
PYRAZOLOPYRIMIDINES AS KINASE INHIBITORS
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Page 25, (2010/02/06)
The present invention relates generally to inhibitors of the kinases and more particularly to novel pyrazolopyrimidine compounds.
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.
