Synthesis and Biological Evaluation of Novel β-Carbolines as Potent Cytotoxic and DNA Intercalating Agents

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概要

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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.

著者

• Yu Liang

  School of Chemistry and Chemical Engineering, Sun Yat-sen University

• Cao Rihui

  School of Chemistry and Chemical Engineering, Sun Yat-sen University

• Yi Wei

  School of Chemistry and Chemical Engineering, Sun Yat-sen University

• Chen Zhiyong

  School of Chemistry and Chemical Engineering, Sun Yat-sen University

• Song Huacan

  School of Chemistry and Chemical Engineering, Sun Yat-sen University

• Shi Buxi

  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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