1.
Bioorg Med Chem Lett
; 23(22): 6192-6, 2013 Nov 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-24095090
RESUMO
The synthesis of bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines is described and their structure-activity-relationship to anaplastic lymphoma kinase (ALK) is presented. KRCA-0008 is selective and potent to ALK and Ack1, and displays drug-like properties without hERG liability. KRCA-0008 demonstrates in vivo efficacy comparable to Crizotinib in xenograft mice model.