A series of novel N-（substituted benzyl）-3,5-bis（benzylidene）-4-piperidones 5a--50 were synthesized with substituted benzylamines as raw materials via a series of Michael addition, Dieckmann condensation, hydrolys...A series of novel N-（substituted benzyl）-3,5-bis（benzylidene）-4-piperidones 5a--50 were synthesized with substituted benzylamines as raw materials via a series of Michael addition, Dieckmann condensation, hydrolysis decarboxylation and aldol condensation. The structures were confirmed by 1↑H NMR, IR, MS techniques and elemental analysis. Assay-based antiproliferative activity study using leukemic cell lines K562 revealed that most of the title compounds have high effectiveness in inhibiting leukemia K562 cells proliferation, among which the compounds 5g （IC50=7.81 μg·mL^-1）, 5k （IC50=6.35μg·mL^-1）, 51 （IC50=7.20 μg·mL^-1）, and 50 （IC50=5.79 μg·mL^-1） have better inhibition activities than standard 5-fluorouracil （IC50=8.56 μg·mL^-1）.展开更多
文摘A series of novel N-（substituted benzyl）-3,5-bis（benzylidene）-4-piperidones 5a--50 were synthesized with substituted benzylamines as raw materials via a series of Michael addition, Dieckmann condensation, hydrolysis decarboxylation and aldol condensation. The structures were confirmed by 1↑H NMR, IR, MS techniques and elemental analysis. Assay-based antiproliferative activity study using leukemic cell lines K562 revealed that most of the title compounds have high effectiveness in inhibiting leukemia K562 cells proliferation, among which the compounds 5g （IC50=7.81 μg·mL^-1）, 5k （IC50=6.35μg·mL^-1）, 51 （IC50=7.20 μg·mL^-1）, and 50 （IC50=5.79 μg·mL^-1） have better inhibition activities than standard 5-fluorouracil （IC50=8.56 μg·mL^-1）.
