Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379698 | Bioorganic & Medicinal Chemistry Letters | 2005 | 4 Pages |
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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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
James J.-W. Duan, Zhonghui Lu, Zelda R. Wasserman, Rui-Qin Liu, Maryanne B. Covington, Carl P. Decicco,