Article ID Journal Published Year Pages File Type
1372115 Bioorganic & Medicinal Chemistry Letters 2010 5 Pages PDF
Abstract

A novel series of TNF-α convertase (TACE) inhibitors which are non-hydroxamate have been discovered. These compounds are bis-amides of l-tartaric acid (tartrate) and coordinate to the active site zinc in a tridentate manner. They are selective for TACE over other MMP’s. We report the first X-ray crystal structure for a tartrate-based TACE inhibitor.

Graphical abstractSynthesis and optimization of novel tartrate TACE inhibitors are described.Figure optionsDownload full-size imageDownload as PowerPoint slide

Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Authors
, , , , , , , , , , , , , , , ,