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Bioorg Med Chem Lett
; 21(8): 2255-8, 2011 Apr 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21429745
RESUMEN
The discovery and hit-to-lead exploration of a novel series of selective IKK-ß kinase inhibitors is described. The initial lead fragment 3 was identified by pharmacophore-directed virtual screening. Homology model-driven SAR exploration of the template led to potent inhibitors, such as 12, which demonstrate efficacy in cellular assays and possess encouraging developability profiles.