Alpha,beta-unsaturated N-acylpyrrole peptidyl derivatives: new proteasome inhibitors.
Basic Information
ID: ALA1240495
Journal: J Med Chem
Title: Alpha,beta-unsaturated N-acylpyrrole peptidyl derivatives: new proteasome inhibitors.
Authors: Baldisserotto A, Ferretti V, Destro F, Franceschini C, Marastoni M, Gavioli R, Tomatis R.
Abstract: 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. N-Acylpyrrole moiety is a potential substrate for Michael addition by catalytic threonine. Several analogues have demonstrated a selective inhibition of the multicatalytic complex beta1 subunits, the capacity to permeate cellular membrane, and good pharmacokinetics properties.
CiteXplore: 20687609
DOI: 10.1021/jm100122e
Patent ID: ┄