N‐(Substituted benzyl)‐3,5‐bis(benzylidene)‐4‐piperidones: Synthesis and Preliminary Anti‐leukemia Activity (I) |
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Authors: | Jing Wang Wen Meng Zhenjie Ni Sijia Xue |
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Affiliation: | Department of Chemistry, College of Life and Environmental Science, Shanghai Normal University, Shanghai 200234, China |
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Abstract: | A series of novel N‐(substituted benzyl)‐3,5‐bis(benzylidene)‐4‐piperidones 5a – 5o 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 1H 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=6.35 µg·mL−1), 5l (IC50=7.20 µg·mL−1), and 5o (IC50=5.79 µg·mL−1) have better inhibition activities than standard 5‐fluorouracil (IC50=8.56 µg·mL−1). |
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Keywords: | 4‐piperidone synthesis inhibition leukemia K562 cell MTT |
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