Article ID Journal Published Year Pages File Type
1379595 Bioorganic & Medicinal Chemistry Letters 2005 5 Pages PDF
Abstract

The application of a tricyclic pyrrolopyrimidinone scaffold for the synthesis of peptidomimetic inhibitors of interleukin-1β-converting enzyme (ICE) is reported. The synthesis of the tricyclic scaffold and conversion of it to a variety of target ICE inhibitors were accomplished in 4–5 steps. In vitro biological evaluation of the tricyclic pyrrolopyrimidinones revealed fair to good ICE inhibitors, with the most active compound exhibiting an IC50 of 14 nM in a caspase-1 enzyme binding assay.

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Physical Sciences and Engineering Chemistry Organic Chemistry
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