| Autor: |
Soper DL; Procter & Gamble Pharmaceuticals, Mason, OH 45040, USA., Sheville J, O'Neil SV, Wang Y, Laufersweiler MC, Oppong KA, Wos JA, Ellis CD, 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 Aug 15; Vol. 16 (16), pp. 4233-6. Date of Electronic Publication: 2006 Jun 16. |
| DOI: |
10.1016/j.bmcl.2006.05.076 |
| Abstrakt: |
Novel 1-(2-acylhydrazinocarbonyl)cycloalkyl carboxamides were designed as peptidomimetic inhibitors of interleukin-1beta converting enzyme (ICE). A short synthesis was developed and moderately potent ICE inhibitors were identified (IC(50) values <100 nM). Most of the synthesized examples were selective for ICE versus the related cysteine proteases caspase-3 and caspase-8, although several dual-acting inhibitors of ICE and caspase-8 were identified. Several of the more potent ICE inhibitors were also shown to inhibit IL-1beta production in a whole cell assay (IC(50) < 500 nM). |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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