Design, synthesis and antitumor activity evaluation of 2,4,6-trisubstituted quinazoline derivatives containing piperidine moiety

In this study, 35 novel 2,4,6-trisubstituted quinazoline derivatives were designed and synthesized, and their anti-tumor activity in vitro were preliminarily explored. Among them, compound 19n exhibited the best anti-proliferative activity against MGC-803 cells with an IC50 of 4.61 mu M. Further biological experiments showed that compound 19n could inhibit the cloning formation of MGC-803 cells. DAPI staining and apoptosis experiments showed that compound 19n could induce apoptosis of MGC-803 cells in a concentration-dependent manner, and the cell cycle experiment indicated that compound 19n could also arrest the MGC-803 cell cycle in G(0)/G(1) phase. In addition, the ADME datas of compound 19n was predicted and the potential target of compound 19n was explained through molecular docking [GRAPHICS] .