| Autor: |
Ellis CD; Procter and Gamble Pharmaceuticals Incorporated, 8700 Mason-Montgomery Road, Mason, OH 45040, USA. ellis.cd@pg.com, 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 |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2006 Sep 15; Vol. 16 (18), pp. 4728-32. Date of Electronic Publication: 2006 Jul 25. |
| DOI: |
10.1016/j.bmcl.2006.07.016 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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