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Bioorg Med Chem Lett
; 16(10): 2699-704, 2006 May 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16516466
RESUMEN
A novel series of achiral TNF-alpha converting enzyme (TACE) inhibitors has been discovered. These compounds exhibited activities from 0.35 to 11nM in a porcine TACE assay and inhibited TNF-alpha production in an LPS-stimulated whole blood assay with an IC(50) value of 23nM for the most potent one. They also have excellent selectivities over related metalloproteases including aggrecanases.