Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR)
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- 作者：Robert D. Hubbard ; Nwe Y. Bamaung ; Fabio Palazzo ; Qian Zhang ; Peter Kovar ; Donald J. Osterling ; Xiaoming Hu ; Julie L. Wilsbacher ; Eric F. Johnson ; Jennifer Bouska ; Jieyi Wang ; R ; y L. Bell ; Steven K. D
- 关键词：Insulin-like growth factor receptor (IGF-IR) ; Kinase ; Inhibitor ; Pyrazolo[3 ; 4-d]pyrimidine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：1 October 2007
- 年：2007
- 卷：17
- 期：19
- 页码：5406-5409
- 全文大小：153 K
文摘
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.