2. Academic Validation
  3. Synthesis of 4β-triazole-podophyllotoxin derivatives by azide-alkyne cycloaddition and biological evaluation as potential antitumor agents

Synthesis of 4β-triazole-podophyllotoxin derivatives by azide-alkyne cycloaddition and biological evaluation as potential antitumor agents

  • Eur J Med Chem. 2011 Sep;46(9):4709-14. doi: 10.1016/j.ejmech.2011.07.024.
Hong Chen 1,  Song Zuo,  Xiaochen Wang,  Xiaowei Tang,  Ming Zhao,  Yanling Lu,  Liting Chen,  Jing Liu,  Yongfeng Liu,  Dailin Liu,  Shi Zhang,  Tan Li
Affiliations

Affiliation

  • 1 Pharmacognosy Division, Medical College of Chinese People's Armed Police Force, Tianjin 300162, China. chenhongtian06@yahoo.com.cn
PMID: 21821321 DOI: 10.1016/j.ejmech.2011.07.024
Abstract

A representative synthetic process of derivatizing the natural product podophyllotoxin utilizing the copper-catalyzed azide-alkyne cycloaddition (CuAAC) is described including molecular design, reaction optimization and X-ray structure confirmation. Evaluation of cytotoxicity against human Cancer cell lines (Hela, K562 and K562/A02) using MTT assay proves that these triazole derivatives have good antitumor activities. High activities toward the drug resistant K562/A02 cell line reveal promising future for these derivatives. The rarely prepared 1,5-disubstituted triazole isomers, which would be omitted by the "click chemistry", were found to have superior cytotoxicities to that of the 1,4-disubstituted isomers.

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