Chinese Journal of Organic Chemistry >
Synthesis and Preliminary Anticancer Activity Evaluation of Tetrahydropyrido[4,3-d]dihydropyrimidine-2-one Derivatives
Received date: 2012-06-06
Revised date: 2012-06-27
Online published: 2012-07-04
Supported by
Project supported by the Key Scientific “Twelfth Five-Year” National Technology Support Program (No. 2011BAE06B01-17), and the National Natural Science Foundation of China (Nos. 21042010, 21102092, 30870560).
In search of more effective anticancer agents, sixteen novel tetrahydropyrido[4,3-d]dihydropyrimidine-2-one derivatives 2a~2p were synthesized by reacting N-(4-substituted benzyl)-3,5-bisbenzylidene-4-piperidone with urea in EtONa/EtOH under reflux condition. The structures were confirmed by 1H NMR, IR, MS and elemental analysis. The preliminary bioassay indicated that some title compounds exhibited good antiproliferative activities against K562 cells, certain antiproliferative activities against ovarian cancer HO-8910 cells and liver cancer SMMC-7721 cells.
Wang Jing , Ding Li , Xiao Di , Xue Sijia . Synthesis and Preliminary Anticancer Activity Evaluation of Tetrahydropyrido[4,3-d]dihydropyrimidine-2-one Derivatives[J]. Chinese Journal of Organic Chemistry, 2012 , 32(11) : 2187 -2192 . DOI: 10.6023/cjoc201206006
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