Article ID Journal Published Year Pages File Type
1379698 Bioorganic & Medicinal Chemistry Letters 2005 4 Pages PDF
Abstract

New inhibitors of tumor necrosis factor-α converting enzyme (TACE) were discovered with a pyrimidine-2,4,6-trione in place of the commonly used hydroxamic acid. These non-hydroxamate TACE inhibitors were developed by incorporating a 4-(2-methyl-4-quinolinylmethoxy)phenyl group, an optimized TACE selective P1′ group. Several leads were identified with IC50 values around 100 nM in a porcine TACE assay and selective over MMP-1, -2, -9, -13, and aggrecanase.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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