Optimization of 4,6-bis-anilino-1H
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- 作者：Stanley D. Chamberlain ; Anikó ; M. Redman ; Joseph W. Wilson ; Felix De ; a ; J. Brad Shotwell ; Roseanne Gerding ; Huangshu Lei ; Bin Yang ; Kirk L. Stevens ; Anne M. Hassell ; Lisa M. Shewchuk ; M. Anthony L
- 关键词：IGF-1R ; IGF-IR ; JNK ; Pyrrolopyrimidine
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：15 January 2009
- 年：2009
- 卷：19
- 期：2
- 页码：360-364
- 全文大小：348 K
文摘
The SAR of C5′ functional groups with terminal basic amines at the C6 aniline of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines is reported. Examples demonstrate potent inhibition of IGF-1R with 1000-fold selectivity over JNK1 and 3 in enzymatic assays.