Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375853 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
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.
Graphical abstractThe 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 in enzymatic and cellular assays with 1000-fold selectivity over JNK1 and 3.Figure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Stanley D. Chamberlain, Anikó M. Redman, Joseph W. Wilson, Felix Deanda, J. Brad Shotwell, Roseanne Gerding, Huangshu Lei, Bin Yang, Kirk L. Stevens, Anne M. Hassell, Lisa M. Shewchuk, M. Anthony Leesnitzer, Jeffery L. Smith, Peter Sabbatini,