1. State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Medical University, Guiyang 550014, China; 2. Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences,Guiyang 550014, China
Abstract：OBJECTIVE To search for and synthesize series of novel anti-tumor quinazoline derivatives.METHODS A series of 4-amino-2-trifluoromethyl quinazoline derivatives were synthesized by condensation, cyclization, chlorination and coupling reaction starting from 2-aminobenzamide.Their anti-proliferative activity against A549, Hela, K562, PC-3 and LNCaPcell lines were evaluated by MTT assay.RESULTS Compound 5c exhibited certain inhibitory activity against PC-3 cell line with inhibitory values of 49.3% at 5 μmol·L-1. The inhibition rate of 6a against LNCaP and K562 was higher than 50.0%as well as compound 6b against PC-3.CONCLUSION Some of the target compounds show certain inhibitory activities against LNCaP, PC-3 and Hela tumor cell lines. In particular, the anti-tumor activities of N-methylated products 6a and 6b are significantly higher than those of the prototype compounds(5n and 5u), which provides a basis for the further study of these compounds.
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2022, Vol. 57 
