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Eur J Med Chem. 2014 Mar 21;75:297-300. doi: 10.1016/j.ejmech.2013.12.044. Epub 2014 Jan 8.

Synthesis and antitumor activity evaluation of chrysin derivatives.

Author information

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.

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

PMID:
24556144
DOI:
10.1016/j.ejmech.2013.12.044
[Indexed for MEDLINE]
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