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

Autor:	David Lindsey Soper, John August Wos, Kofi A. Oppong, Richard L. Wang, Biswanath De, Laufersweiler Michael Christopher, Thomas P. Demuth, Wei Lu, Steven V. O’Neil, Maureen K. Suchanek, Christopher D. Ellis, Amy N. Fancher, Yili Wang
Rok vydání:	2006
Předmět:	Models Molecular Thiazepines Peptidomimetic Stereochemistry medicine.drug_class Clinical Biochemistry Pharmaceutical Science Carboxamide Crystallography X-Ray Biochemistry Chemical synthesis Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Thiazepine Enzyme Inhibitors Molecular Biology IC50 chemistry.chemical_classification Molecular Structure biology Caspase 1 Organic Chemistry Caspase Inhibitors In vitro Enzyme chemistry Enzyme inhibitor biology.protein Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 16:4728-4732
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2006.07.016
Popis:	A series of monocyclic thiazepine inhibitors of interleukin-1β 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:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::22a6295e34134eb99771fc41c3af1397 https://doi.org/10.1016/j.bmcl.2006.07.016 Zobrazit plný text záznamu Full Text from ScienceDirect