Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372865 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
A series of analogs of 3-(2-amino-ethyl)-5-(4-ethoxy-benzylidene)-thiazolidine-2,4-dione, a putative substrate-specific ERK1/2 inhibitor, were synthesized and biologically characterized in human leukemia U937 cells to define its pharmacophore. It was discovered that shift of ethoxy substitution from the 4- to the 2-position on the phenyl ring significantly improved functional activities of inhibiting cell proliferation and inducing apoptosis. This may provide access to a new lead for developing ERK1/2 substrate-specific inhibitors.
Graphical abstractPreliminary structure–activity relationship studies of 3-(2-amino-ethyl)-5-(4-ethoxy-benzylidene)-thiazolidine-2,4-dione, a putative substrate-specific ERK1/2 inhibitor, is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide