title: Synthesis and antitumor activity evaluation of chrysin derivatives.
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.
authors.affiliation: 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.
authors.forename: Zhen-Yuan
authors.initials: ZY
authors.lastname: Zhu
authors.affiliation: 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.
authors.forename: Wan-Xiao
authors.initials: WX
authors.lastname: Wang
authors.affiliation: 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.
authors.forename: Zhen-qian
authors.initials: ZQ
authors.lastname: Wang
authors.affiliation: Key Laboratory of Freshwater Fishery Germplasm Resources, Ministry of Agriculture, Shanghai Ocean University, 201306, PR China.
authors.forename: Li-Jing
authors.initials: LJ
authors.lastname: Chen
authors.affiliation: 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.
authors.forename: Jing-Yi
authors.initials: JY
authors.lastname: Zhang
authors.affiliation: 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.
authors.forename: Xiao-Cui
authors.initials: XC
authors.lastname: Liu
authors.affiliation: Université Pierre et Marie Curie-Paris 6, Institut Parisien de Chimie Moléculaire UMR CNRS 7201, 4 place Jussieu, 75005, Paris, France.
authors.forename: Shao-ping
authors.initials: SP
authors.lastname: Wu
authors.affiliation: Université Pierre et Marie Curie-Paris 6, Institut Parisien de Chimie Moléculaire UMR CNRS 7201, 4 place Jussieu, 75005, Paris, France.
authors.forename: Yong-Min
authors.initials: YM
authors.lastname: Zhang
mesh_terms: D000107:Acetylation; D000478:Alkylation; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D005419:Flavonoids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D016195:G2 Phase / Q000187:drug effects; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy
chemical_list: D000970:Antineoplastic Agents; D005419:Flavonoids; C043561:chrysin
keywords: Active sites; Antitumor agents; Chrysin derivatives; H22; Inhibition of cell division