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Updated: Aug 6, 2026

Evaluation of the In vivo Antitumor Activity of Polyanhydride IL-1α Nanoparticles
Published on: June 28, 2021
Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors
Christopher D Ellis1, Kofi A Oppong, Michael C Laufersweiler
1Procter and Gamble Pharmaceuticals Incorporated, 8700 Mason-Montgomery Road, Mason, OH 45040, USA. ellis.cd@pg.com
Abstract:
A series of monocyclic thiazepine inhibitors of interleukin-1beta 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.