Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: Potent inhibitors of the IGF-1R receptor tyrosine kinase

The evaluation of a series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines as inhibitors of the IGF-1R (IGF-IR) receptor tyrosine kinase is reported. Examples demonstrate nanomolar potencies in in vitro enzyme and mechanistic cellular assays as well as promising in vivo pharmacokinetics in rat.

A series of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines are evaluated as IGF-1R inhibitors. Reported examples demonstrate nanomolar potencies in in vitro enzyme and cellular assays as well as promising in vivo pharmacokinetics in rat.Figure optionsDownload as PowerPoint slide