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ID: ALA1147697
Journal: Bioorg Med Chem Lett
Title: Synthesis and structure-activity relationship of a novel, achiral series of TNF-alpha converting enzyme inhibitors.
Authors: Gilmore JL, King BW, Harris C, Maduskuie T, Mercer SE, Liu RQ, Covington MB, Qian M, Ribadeneria MD, Vaddi K, Trzaskos JM, Newton RC, Decicco CP, Duan JJ.
Abstract: 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.
CiteXplore: 16516466