1.
Bioorg Med Chem Lett
; 16(17): 4686-91, 2006 Sep 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16777410
RESUMEN
Synthetic modifications on a 6-furanylquinazoline scaffold to optimize the dual ErbB-1/ErbB-2 tyrosine kinase inhibition afforded consistent SAR whereby a 4-(3-fluorobenzyloxy)-3-haloanilino provided the best enzyme potency and cellular selectivity. Changes made to the 6-furanyl group had little impact on the enzyme activity, but appeared to dramatically affect the cellular efficacy. The discovery of lapatinib emerged from this work.