Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 55, Issue 10, Pages 4872-4876Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm3003944
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Funding
- European Commission [043310]
- Percy Falk's foundation
- Swedish Cancer Fund [10-0633]
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A series of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines have been designed, synthesized, and evaluated as RET protein kinase inhibitors. On the basis of docking results, a small library of pyrazolopyrimidine compounds with an extended hydrophobic side arm was synthesized. The most promising of the compounds (7a) displayed efficient inhibition in vitro and good selectivity when tested on a panel of kinases. Furthermore, 7a inhibited GDNF-induced RET phosphorylation of ERK1/2 in MCF-7 breast cancer cells at concentrations as low as 100 nM.
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