Title of article
Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: Inhibition of interleukin-1β-converting enzyme
Author/Authors
Michael C. Laufersweiler، نويسنده , , Yili Wang، نويسنده , , David L. Soper، نويسنده , , Maureen K. Suchanek، نويسنده , , Amy N. Fancher، نويسنده , , Wei Lu، نويسنده , , Richard L. Wang، نويسنده , , Kofi A. Oppong، نويسنده , , Christopher D. Ellis، نويسنده , , Mark W. Baize، نويسنده , , Steven V. O’Neil، نويسنده , , John A. Wos، نويسنده , , Thomas P. Demuth Jr.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2005
Pages
5
From page
4322
To page
4326
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.
Keywords
Pyrrolopyrimidinones , Caspase-1 , Heterocycles , Interleukin-1?-converting enzyme , Peptidomimitics
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2005
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795985
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