Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR)

A high throughput screen of Abbott’s compound repository revealed that the pyrazolo[3,4-d]pyrimidine class of kinase inhibitors possessed moderate potency for IGF-IR, a promising target for cancer chemotherapy. The synthesis and subsequent optimization of this class of compounds led to the discovery of 14, a compound that possesses in vivo IGF-IR inhibitory activity.

Graphical abstractThe synthesis, in vitro and in vivo characterization of a novel class of insulin-like growth factor receptor tyrosine kinase inhibitors, the pyrazolo[3,4-d]pyrimidines, is disclosed.Figure optionsDownload full-size imageDownload as PowerPoint slide