1.
Bioorg Med Chem Lett
; 11(20): 2775-8, 2001 Oct 22.
Artigo
em Inglês
| MEDLINE
| ID: mdl-11591521
RESUMO
Heterocyclic ureas, such as N-3-thienyl N'-aryl ureas, have been identified as novel inhibitors of raf kinase, a key mediator in the ras signal transduction pathway. Structure-activity relationships were established, and the potency of the screening hit was improved 10-fold to IC(50)=1.7 microM. A combinatorial synthesis approach enabled the identification of a breakthrough lead (IC(50)=0.54 microM) for a second generation series of heterocyclic urea raf kinase inhibitors.