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

  • Bioorg Med Chem Lett. 2007 Oct 1;17(19):5406-9. doi: 10.1016/j.bmcl.2007.07.037.
Robert D Hubbard  1 ,  Nwe Y Bamaung ,  Fabio Palazzo ,  Qian Zhang ,  Peter Kovar ,  Donald J Osterling ,  Xiaoming Hu ,  Julie L Wilsbacher ,  Eric F Johnson ,  Jennifer Bouska ,  Jieyi Wang ,  Randy L Bell ,  Steven K Davidsen ,  George S Sheppard
Affiliations
  • 1. Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA. [email protected]
PMID: 17689078 DOI: 10.1016/j.bmcl.2007.07.037
Abstract

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.