2. Academic Validation
  3. Synthesis and antitumor activity evaluation of chrysin derivatives

Synthesis and antitumor activity evaluation of chrysin derivatives

  • Eur J Med Chem. 2014 Mar 21:75:297-300. doi: 10.1016/j.ejmech.2013.12.044.
Zhen-Yuan Zhu 1,  Wan-Xiao Wang 2,  Zhen-qian Wang 2,  Li-Jing Chen 3,  Jing-Yi Zhang 2,  Xiao-Cui Liu 2,  Shao-ping Wu 4,  Yong-Min Zhang 4
Affiliations

Affiliations

  • 1 Key Laboratory of Food Nutrition and Safety, Ministry of Education, College of Food Science and Biotechnology, Tianjin University of Science and Technology, Tianjin 300457, PR China. Electronic address: zhyuanzhu@tust.edu.cn.
  • 2 Key Laboratory of Food Nutrition and Safety, Ministry of Education, College of Food Science and Biotechnology, Tianjin University of Science and Technology, Tianjin 300457, PR China.
  • 3 Key Laboratory of Freshwater Fishery Germplasm Resources, Ministry of Agriculture, Shanghai Ocean University, 201306, PR China.
  • 4 Université Pierre et Marie Curie-Paris 6, Institut Parisien de Chimie Moléculaire UMR CNRS 7201, 4 place Jussieu, 75005, Paris, France.
PMID: 24556144 DOI: 10.1016/j.ejmech.2013.12.044
Abstract

A series of 5,7-disubstituted chrysin, 7-monosubstituted chrysin, 5-monosubstituted chrysin derivatives were synthesized by alkylation, acetylation, benzoylation, carboxymethylation, and evaluated on their antitumor activity of H22 cells in the search for potential antitumor agents. Among them, compound 3 (5,7-diacetyl chrysin) displayed the most potent antitumor activity with IC50 value of 141 μM. Moreover, there is significant up-regulation of G2 in cell cycle of H22.

Keywords

Active sites; Antitumor agents; Chrysin derivatives; H22; Inhibition of cell division.

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