1095314-05-8Relevant articles and documents
Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases
Xu, Guozhang,Searle, Lily Lee,Hughes, Terry V.,Beck, Amanda K.,Connolly, Peter J.,Abad, Marta C.,Neeper, Michael P.,Struble, Geoffrey T.,Springer, Barry A.,Emanuel, Stuart L.,Gruninger, Robert H.,Pandey, Niranjan,Adams, Mary,Moreno-Mazza, Sandra,Fuentes-Pesquera, Angel R.,Middleton, Steven A.,Greenberger, Lee M.
scheme or table, p. 3495 - 3499 (2009/04/11)
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 IC50 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.
