Pyrazolo-quinolinones is a new class of compounds with anti-tumor,anti-oxidation and other biological activities,which has a good medicinal prospect.However,there are few reports on the syntheses and biological activities of these compounds.In this paper,eight pyrazolo-quinolinones derivatives(a～h)have been prepared by a three-component"one-pot"reaction,and their cytotoxic activities were evaluated.The results showed that the compounds exhibited good selective cytotoxic activity against tumor cell lines(Hela,HCC1806 and A549),especially compound h showed the best inhibitory effect on A549(IC50=1.31 μmol/L).In addition,the molecular docking study indicated that compound h had a strong interaction with the target protein 4PTC,which could be considered as potential glycogen synthase kinase-3 inhibitor for further study.
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