Synthesis and biological evaluation of novel β-carbolines as potent cytotoxic and DNA intercalating agents

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  • Chen Zhiyong
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Cao Rihui
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Shi Buxi
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Yi Wei
    School of Chemistry and Chemical Engineering, Sun Yat-sen University Departement de Pharmacochimie Moleculaire, UMR-CNRS 5063, Faculte de Pharmacie de Grenoble
  • Yu Liang
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Song Huacan
    School of Chemistry and Chemical Engineering, Sun Yat-sen University
  • Ren Zhenhua
    State Key Laboratory of Biocontrol, School of Life Science, Sun Yat-sen University

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タイトル別名
  • Synthesis and Biological Evaluation of Novel .BETA.-Carbolines as Potent Cytotoxic and DNA Intercalating Agents
  • Synthesis and biological evaluation of novel v carbolines as potent cytotoxic and DNA intercalating agents

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A series of novel water-soluble β-carbolines bearing a flexible amino side chain was designed, synthesized and evaluated as potent cytotoxic and DNA intercatalating agents. The N9-arylated alkyl substituted β-carbolines represented the most interesting cytotoxic activities. The results suggested that (1) the N9-arylated alkyl substituents of β-carboline nucleus played a very important role in the modulation of the cytotoxic potencies; (2) the length of the alkylamino side chain significantly affected their cytotoxic potency, and N,N-dimethylaminopropylamino substituent were more favorable. In addition, these compounds were found to exhibit significant DNA intercalating potencies.

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