Interleukin-1β converting enzyme : synthesis of hydroxyethyl dipeptide surrogate-containing compounds as potential ICE inhibitors

摘要: A series of compounds containing a hydroxyethyl-based dipeptide surrogate have been prepared as probes to evaluate the possibility ICE being an aspartic protease. The aldehyde t-BocAsp(beta-t-butyl)H reacted with organochromium species derived from phenethyl bromide and CrCl2 give expected addition product. Lactonization, reprotection amine oxidation RuCl3 gave two protected surrogates 7a 7b. These were incorporated into tetra-, penta- hexapeptide-like molecules evaluated inhibitors enzyme. failure these inhibit indicated that this enzyme was very unlikely be