1.
Bioorg Med Chem Lett
; 18(12): 3495-9, 2008 Jun 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18508264
RESUMEN
We herein disclose a novel series of 4-aminopyrimidine-5-carbaldehyde oximes that are potent and selective inhibitors of both EGFR and ErbB-2 tyrosine kinases, with IC(50) values in the nanomolar range. Structure-activity relationship (SAR) studies elucidated a critical role for the 4-amino and C-6 arylamino moieties. The X-ray co-crystal structure of EGFR with 37 was determined and validated our design rationale.