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, 19 (2), 360-4

Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R Tyrosine Kinase Inhibitors Towards JNK Selectivity

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Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R Tyrosine Kinase Inhibitors Towards JNK Selectivity

Stanley D Chamberlain et al. Bioorg Med Chem Lett.

Abstract

The SAR of C5' functional groups with terminal basic amines at the C6 aniline of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidines is reported. Examples demonstrate potent inhibition of IGF-1R with 1000-fold selectivity over JNK1 and 3 in enzymatic assays.

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