Guozhang Xu, L. L. Searle, T. V. Hughes
Jun 15, 2008
Citations
1
Influential Citations
46
Citations
Journal
Bioorganic & medicinal chemistry letters
Abstract
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.