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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.

Patnaik S., Stevens K.L., Gerding R., Deanda F., Shotwell J.B., Tang J., Hamajima T., Nakamura H., Leesnitzer M.A., Hassell A.M., Shewchuck L.M., Kumar R., Lei H., Chamberlain S.D.

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.

Bioorg. Med. Chem. Lett. 19:3136-3140(2009) [PubMed] [Europe PMC]