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.
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Patnaik S, Stevens KL, Gerding R, Deanda F, Shotwell JB, Tang J, Hamajima T, Nakamura H, Leesnitzer MA, Hassell AM, Shewchuck LM, Kumar R, Lei H, Chamberlain SD
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.
Bioorg Med Chem Lett. 2009 Jun 1;19(11):3136-40. doi: 10.1016/j.bmcl.2008.12.110. Epub 2009 Jan 6.
- PubMed ID
- 19394223 [ View in PubMed]
- Abstract
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.