This research is about the integration of two anti-tumor structures, which are 1,8-naphthyridinones and aminopyrimidines, designing novel tetrahydroquinazolines (TQ) derivatives and confering a series of TQ derivatives. Preliminary results showed that the introduction of 3-chlorophenyl and 4-chlorophenyl into 2-position of amino group on TQ increased the activity against chondrosarcoma (JJ). Moreover, the replacement of 5-carbonyl group with hydroxyamine group dramatically enhanced the anti-chondrosarcoma activity. To the anti-inflammatory study, we focus on the structure-activity relationship of TQ for the effect of N-formyl-methionyl-leucylphenylalanine (fMLP) in human neutrophils induced by superoxide anion (O2•−) generation in human neutrophils. Preliminary results showed that the introduction of 2-chlorophenyl and 2-fluorophenyl into 2-position of amino group on TQ increased the activity against inflammatory. The same, replace the 5 - carbonyl and hydroxyamine group significantly increased the activities of the anti-inflammatory.
