Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors.

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Ellis CD, Oppong KA, Laufersweiler MC, O'Neil SV, Soper DL, Wang Y, Wos JA, Fancher AN, Lu W, Suchanek MK, Wang RL, De B, Demuth TP Jr

Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4728-32. Epub 2006 Jul 25.

PubMed ID

16870441 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Pralnacasan	Caspase-1	IC 50 (nM)	3.6	N/A	N/A	Details