Optimization of 4,6-bis-anilino-1H-pyrrolo[2,3-d]pyrimidine IGF-1R tyrosine kinase inhibitors towards JNK selectivity.

Abstract The SAR of C5′ functional groups with terminal basic amines at the C6 aniline of 4,6-bis-anilino-1 H -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.