Bioorganic & medicinal chemistry letters, 2005-10, Vol.15 (19), p.4322
2005
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Details
- Autor(en) / Beteiligte
- Titel
- Synthesis and evaluation of tricyclic pyrrolopyrimidinones as dipeptide mimetics: inhibition of interleukin-1beta-converting enzyme
- Ist Teil von
- Bioorganic & medicinal chemistry letters, 2005-10, Vol.15 (19), p.4322
- Ort / Verlag
- England
- Erscheinungsjahr
- 2005
- Quelle
- Access via ScienceDirect (Elsevier)
- Beschreibungen/Notizen
- The application of a tricyclic pyrrolopyrimidinone scaffold for the synthesis of peptidomimetic inhibitors of interleukin-1beta-converting enzyme (ICE) is reported. The synthesis of the tricyclic scaffold and conversion of it to a variety of target ICE inhibitors were accomplished in 4-5 steps. In vitro biological evaluation of the tricyclic pyrrolopyrimidinones revealed fair to good ICE inhibitors, with the most active compound exhibiting an IC50 of 14 nM in a caspase-1 enzyme binding assay.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0960-894XTitel-ID: cdi_pubmed_primary_16046129
- Format
- –
- Schlagworte
- Caspase Inhibitors, Dipeptides - chemical synthesis, Dipeptides - pharmacology, Enzyme Inhibitors - chemical synthesis, Enzyme Inhibitors - pharmacology, Heterocyclic Compounds, 3-Ring - chemical synthesis, Heterocyclic Compounds, 3-Ring - pharmacology, Humans, Immunologic Factors - chemical synthesis, Immunologic Factors - pharmacology, Inhibitory Concentration 50, Molecular Mimicry, Monocytes, Pyrimidinones - chemical synthesis, Pyrimidinones - pharmacology, Pyrroles - chemical synthesis, Pyrroles - pharmacology, Structure-Activity Relationship