Title of article
Synthesis and evaluation of thiazepines as interleukin-1β converting enzyme (ICE) inhibitors
Author/Authors
Christopher D. Ellis، نويسنده , , Kofi A. Oppong، نويسنده , , Michael C. Laufersweiler، نويسنده , , Steven V. O’Neil، نويسنده , , David L. Soper، نويسنده , , Yili Wang، نويسنده , , John A. Wos، نويسنده , , Amy N. Fancher، نويسنده , , Wei Lu، نويسنده , , Maureen K. Suchanek، نويسنده , , Richard L. Wang، نويسنده , , Biswanath De، نويسنده , , Thomas P. Demuth Jr.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
4728
To page
4732
Abstract
A series of monocyclic thiazepine inhibitors of interleukin-1β converting enzyme (ICE) were synthesized in eight steps from commercially available intermediates. In vitro biological evaluation showed the thiazepines to be moderately potent ICE inhibitors, with the most active compound exhibiting an IC50 value of 30 nM in an enzyme inhibition assay. Compounds of this class possessed good selectivity against the related enzymes caspase-3 and caspase-8.
Keywords
Caspase-1 , Peptidomimetic , Interleukin-1? , Thiazepine , ICE
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797264
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