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Bioorg Med Chem Lett
; 23(22): 6192-6, 2013 Nov 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-24095090
RESUMEN
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.