期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 75, 期 -, 页码 297-300出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.12.044
关键词
Chrysin derivatives; Antitumor agents; H22; Active sites; Inhibition of cell division
资金
- National Agricultural Innovation Project [2011GB2A100009]
- Foundation of Tianjin University of Science and Technology [20120106]
- International Science & Technology Cooperation Program of China [2013DFA31160]
- National Spark Program of China [2012GA610005]
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 mu M. Moreover, there is significant up-regulation of G2 in cell cycle of H22. (C) 2014 Elsevier Masson SAS. All rights reserved.
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