Discovery of 4,6-bis-anilino-1H
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- 作者：Stanley D. Chamberlain ; Joseph W. Wilson ; Felix De ; a ; Samarjit Patnaik ; Anikó ; M. Redman ; Bin Yang ; Lisa Shewchuk ; Peter Sabbatini ; M. Anthony Leesnitzer ; Arthur Groy ; Charity Atkins ; Roseanne Ger
- 关键词：Pyrrolopyrimidine ; IGF-1R ; Kinase inhibitor ; IGF-IR
- 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：469-473
- 全文大小：274 K
文摘
The evaluation of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines as inhibitors of the IGF-1R (IGF-IR) receptor tyrosine kinase is reported. Examples demonstrate nanomolar potencies in in vitro enzyme and mechanistic cellular assays as well as promising in vivo pharmacokinetics in rat.