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.
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; Moorthy, G; Rowand, JL; Stevens, KL; Kumar, R; Shotwell, JB
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