Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase.
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Chamberlain SD, Wilson JW, Deanda F, Patnaik S, Redman AM, Yang B, Shewchuk L, Sabbatini P, Leesnitzer MA, Groy A, Atkins C, Gerding R, Hassell AM, Lei H, Mook RA Jr, Moorthy G, Rowand JL, Stevens KL, Kumar R, Shotwell JB
Discovery of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines: potent inhibitors of the IGF-1R receptor tyrosine kinase.
Bioorg Med Chem Lett. 2009 Jan 15;19(2):469-73. doi: 10.1016/j.bmcl.2008.11.046. Epub 2008 Nov 18.
- PubMed ID
- 19056263 [ View in PubMed]
- Abstract
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.