α,β-Unsaturated <i>N</i>-Acylpyrrole Peptidyl Derivatives: New Proteasome Inhibitors Anna Baldisserotto Valeria Ferretti Federica Destro Christian Franceschini Mauro Marastoni Riccardo Gavioli Roberto Tomatis 10.1021/jm100122e.s001 https://acs.figshare.com/articles/journal_contribution/_Unsaturated_i_N_i_Acylpyrrole_Peptidyl_Derivatives_New_Proteasome_Inhibitors/2732047 Because of the encouraging results obtained using vinyl ester derivatives, we synthesized and tested a novel series of peptide-based proteasome inhibitors bearing a new pharmacophore unit at the C-terminal. <i>N</i>-Acylpyrrole moiety is a potential substrate for Michael addition by catalytic threonine. Several analogues have demonstrated a selective inhibition of the multicatalytic complex β1 subunits, the capacity to permeate cellular membrane, and good pharmacokinetics properties. 2010-09-09 00:00:00 vinyl ester derivatives Derivative moiety capacity Michael addition multicatalytic pharmacophore unit pharmacokinetics properties membrane Several analogues proteasome Peptidyl β1 subunits inhibition threonine substrate New Proteasome InhibitorsBecause novel series inhibitor Unsaturated