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Bioorg Med Chem Lett. 2009 Jan 15;19(2):469-73. doi: 10.1016/j.bmcl.2008.11.046. Epub 2008 Nov 18.

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

Author information

1
GlaxoSmithKline, Oncology R&D, 5 Moore Drive, 3.4184.4B, PO Box 13398, Research Triangle Park, NC 27709-3398, USA.

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.

PMID:
19056263
DOI:
10.1016/j.bmcl.2008.11.046
[Indexed for MEDLINE]

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