A novel structural class of potent inhibitors of NF-κB activation: structure–activity relationships and biological effects of 6-aminoquinazoline derivatives
In this study, we have investigated the roles of substituents on the terminal phenyl ring at the C (4)-position of the quinazoline core to complete the structure–activity relationships (SARs) of our NF-κB activation inhibitors. Among them, compound 12j afforded highly potent inhibitory activity toward NF-κB transcriptional activation with IC50 value of 2nM, along with an excellent in vivo efficacy by reducing the edema formation seen in carrageenin- ...