吡唑并[3,4-d]嘧啶作为胰岛素样生长因子受体（IGF-IR）的强效抑制剂。
Pyrazolo[3,4-d]pyrimidines as potent inhibitors of the insulin-like growth factor receptor (IGF-IR).
作者信息
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
机构信息
Cancer Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA.
出版信息
Bioorg Med Chem Lett. 2007 Oct 1;17(19):5406-9. doi: 10.1016/j.bmcl.2007.07.037. Epub 2007 Jul 25.
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.
对雅培化合物库进行的高通量筛选显示，吡唑并[3,4-d]嘧啶类激酶抑制剂对IGF-IR具有中等效力，IGF-IR是癌症化疗中一个很有前景的靶点。这类化合物的合成及后续优化导致了化合物14的发现，该化合物具有体内IGF-IR抑制活性。
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