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- W2389452011 abstract "Objective To investigate the structure-activity relationship of anti-tumor activities and the corresponding mechanism of 13-substituted berberine derivatives.Methods Berberine was used as the starting material,13-alkyl berberine derivatives were gained by a selective reduction followed by the reaction with fatty aldehyde,while 13-ben zyl berberine derivatives were prepared by an additional reaction with acetone in basic condition followed by the reac tion with various substituted benzyl bromides.SRB assay was used to detect anti-tumor activities and the flow cytome try assay was used to analyze the effect on cell cycle distribution induced by the compounds.Results 14 target compounds were designed and synthesized in this study,7 of them were novel compounds,and their structures were deter mined by 1H-NMR and high resolution mass(HRS).All the target compounds showed higher anti-tumor activities than berberine,and especially,compound 3h exhibited the potential anti-cancer activities,on HepG2 and HL60 cells with IC50 values of 0.08 and 0.06 μg/mL,respectively.The primary structure-activity relationship demonstrated that 13 alkyl berberine derivatives showed obviously higher anti-tumor activities than 13-benzyl berberine derivatives,and a moderate length of the alkyl chain was beneficial for the activity.The primary mechanism study showed that cell cycle blockage at G2/M phase in HCT116.Conclusion 13-substituted berberine derivatives are promising as a kind of novel anti-tumor agents." @default.
- W2389452011 created "2016-06-24" @default.
- W2389452011 creator A5060156606 @default.
- W2389452011 date "2013-01-01" @default.
- W2389452011 modified "2023-10-17" @default.
- W2389452011 title "Synthesis and structure-activity relationship of 13-substituted berberine derivatives as anti-cancer agents" @default.
- W2389452011 hasPublicationYear "2013" @default.
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