943975-06-2Relevant academic research and scientific papers
PYRIMIDINE INHIBITORS OF KINASE ACTIVITY
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Page/Page column 63, (2010/12/26)
Described herein are compounds of formula (I) or pharmaceutical acceptable salts or solvates thereof, wherein G1, L1, R2, R3, n, p, Ar1, and Ar2 are defined in the description. Methods of making said compounds, and compositions comprising said compounds which are useful for inhibiting kinases such as IGF-IR are also disclosed.
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.
