862729-83-7Relevant academic research and scientific papers
Development of multitargeted inhibitors of both the insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor family of receptor tyrosine kinases
Hubbard, Robert D.,Bamaung, Nwe Y.,Fidanze, Steve D.,Erickson, Scott A.,Palazzo, Fabio,Wilsbacher, Julie L.,Zhang, Qian,Tucker, Lora A.,Hu, Xiaoming,Kovar, Peter,Osterling, Donald J.,Johnson, Eric F.,Bouska, Jennifer,Wang, Jieyi,Davidsen, Steven K.,Bell, Randy L.,Sheppard, George S.
experimental part, p. 1718 - 1721 (2009/11/30)
Emerging clinical and pre-clinical data indicate that both insulin-like growth factor receptor (IGF-IR) and members of the epidermal growth factor (EGF) family of receptor tyrosine kinases (RTKs) exhibit significant cross-talk in human cancers. Therefore, a small molecule that successfully inhibits the signaling of both classes of oncogenic kinases might provide an attractive agent for chemotherapeutic use. Herein, we disclose the structure activity relationships that led to the synthesis and biological characterization of 14, a novel small molecule inhibitor of both IGF-IR and members of the epidermal growth factor family of RTKs.
Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR)
Hubbard, Robert D.,Bamaung, Nwe Y.,Palazzo, Fabio,Zhang, Qian,Kovar, Peter,Osterling, Donald J.,Hu, Xiaoming,Wilsbacher, Julie L.,Johnson, Eric F.,Bouska, Jennifer,Wang, Jieyi,Bell, Randy L.,Davidsen, Steven K.,Sheppard, George S.
, p. 5406 - 5409 (2008/03/13)
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.
