Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379595 | Bioorganic & Medicinal Chemistry Letters | 2005 | 5 Pages |
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
Authors
Michael C. Laufersweiler, Yili Wang, David L. Soper, Maureen K. Suchanek, Amy N. Fancher, Wei Lu, Richard L. Wang, Kofi A. Oppong, Christopher D. Ellis, Mark W. Baize, Steven V. O’Neil, John A. Wos, Thomas P. Demuth Jr.,