Discovery of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines as potent inhibitors of the insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase

Exploration of the SAR around a series of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of novel pyrrolopyridines as nanomolar inhibitors of the IGF-1R tyrosine kinase. Exploration of the SAR around a series of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-06, Vol.19 (11), p.3136-3140
Hauptverfasser:	Patnaik, Samarjit, Stevens, Kirk L., Gerding, Roseanne, Deanda, Felix, Shotwell, J. Brad, Tang, Jun, Hamajima, Toshihiro, Nakamura, Hiroko, Leesnitzer, M. Anthony, Hassell, Anne M., Shewchuck, Lisa M., Kumar, Rakesh, Lei, Huangshu, Chamberlain, Stanley D.
Format:	Artikel
Sprache:	eng
Schlagworte:	BASIC BIOLOGICAL SCIENCES Drug Design ENZYMES EXPLORATION GENERAL AND MISCELLANEOUS//MATHEMATICS, COMPUTING, AND INFORMATION SCIENCE IGF-1R IGF-IR Kinase inhibitor PHOSPHOTRANSFERASES Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Pyridines - chemical synthesis Pyridines - chemistry Pyridines - pharmacology Pyrroles - chemical synthesis Pyrroles - chemistry Pyrroles - pharmacology Pyrrolopyridine Receptor, IGF Type 1 - antagonists & inhibitors Receptor, IGF Type 1 - metabolism Structure-Activity Relationship TYROSINE
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Zusammenfassung:	Exploration of the SAR around a series of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of novel pyrrolopyridines as nanomolar inhibitors of the IGF-1R tyrosine kinase. Exploration of the SAR around a series of 3,5-disubstituted-1H-pyrrolo[2,3-b]pyridines led to the discovery of novel pyrrolopyridine inhibitors of the IGF-1R tyrosine kinase. Several compounds demonstrated nanomolar potency in enzyme and cellular mechanistic assays.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2008.12.110