Synthesis and Antitumor Activity of N-Pheny1-4-(Trifluoromethyl)-Quinazoline-2-Amine Derivatives
OBJECTIVE To find new arylaminoquinazoline-based antitumor target compounds with high efficacy and low toxicity.METHODS A series of N-phenyl-4-(trifluoromethyl)quinazoline-2-amine derivatives were synthesized starting from 2-nitrobenzalde-hyde or 6-nitroveratraldehyde by a combination of nucleophilic addition,oxidation,reduction,cyclization,chlorination,and coupling re-actions.The structures of the target compounds were characterized using NMR and MS.Their antitumor activities in vitro were then evaluated against four human cancer cell lines(PC3,LNCaP,K562,and HeLa)using MTT assay.The target prediction of active com-pound 8b was performed.RESULTS Compounds 8b and 8c exhibited promising anti-proliferative properties,particularly compound 8b,which exhibited excellent antitumor activity against PC3,LNCaP,and K562 with IC50 values of 5.51,4.51 and 8.49 μmol·L-1,respectively.Molecular docking experiment demonstrated that PIM-1 is the potential target of 8b.CONCLUSION The piperazine ring containing compound 8b exhibits the strongest antitumor activity,which is worthy of further study.
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