Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375856 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
Initial evaluation of a series 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines revealed a C(1′) carboxamide was preferred for sub-micromolar in vitro potency against IGF-1R. Subsequent solution stability studies with 1 revealed a susceptibility toward acid-induced intramolecular cyclization with the C(1′) carboxamide. Herein, we describe several successful approaches toward generating both potent and acid-stable inhibitors of IGF-1R within the 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine template.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Stanley D. Chamberlain, Anikó M. Redman, Samarjit Patnaik, Keith Brickhouse, Yen-Chiat Chew, Felix Deanda, Roseanne Gerding, Huangshu Lei, Ganesh Moorthy, Mark Patrick, Kirk L. Stevens, Joseph W. Wilson, J. Brad Shotwell,