title: Phosphoramidate protides of five flavones and their antiproliferative activity against HepG2 and L-O2 cell lines.
abstract: A series of flavone-7-phosphoramidate derivatives were synthesized and tested for their antiproliferative activity in vitro against human hepatoma cell line HepG2 and human normal hepatic cell line L-O2. Compound 8d, 16d and 17d, incorporating the amino acid alanine, exhibited high inhibitory activity on HepG2 cell line with IC50 values of 9.0 μmol/L, 5.5 μmol/L and 6.6 μmol/L. The introduction of acyl groups played a pivotal role in the selective inhibition toward human hepatoma HepG2 cells, except for compound 8a, 9a and 16b. Compound 8d, 16d and 17d could significantly induce G2/M arrest in HepG2 cells. Specially, Compound 16d could lead early apoptosis in HepG2 cells.
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, 2 Linggong Road, Dalian 116024, China.
authors.forename: Yue-Qing
authors.initials: YQ
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, 2 Linggong Road, Dalian 116024, China.
authors.forename: Fei
authors.initials: F
authors.lastname: Yang
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, 2 Linggong Road, Dalian 116024, China.
authors.forename: Liu
authors.initials: L
authors.lastname: Wang
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, 2 Linggong Road, Dalian 116024, China.
authors.forename: Zhi
authors.initials: Z
authors.lastname: Cao
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, 2 Linggong Road, Dalian 116024, China.
authors.forename: Tian-Jiao
authors.initials: TJ
authors.lastname: Han
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, 2 Linggong Road, Dalian 116024, China.
authors.forename: Zhe-Ang
authors.initials: ZA
authors.lastname: Duan
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, 2 Linggong Road, Dalian 116024, China.
authors.forename: Zhen
authors.initials: Z
authors.lastname: Li
authors.affiliation: School of Pharmaceutical Science and Technology, Dalian University of Technology, 2 Linggong Road, Dalian 116024, China. Electronic address: zyzhao@dlut.edu.cn.
authors.forename: Wei-Jie
authors.initials: WJ
authors.lastname: Zhao
mesh_terms: D000577:Amides / Q000737:chemistry* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D059447:Cell Cycle Checkpoints / Q000187:drug effects; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects*; D047309:Flavones / Q000737:chemistry* / Q000494:pharmacology*; D056945:Hep G2 Cells; D006801:Humans; D008099:Liver / Q000166:cytology / Q000187:drug effects / Q000473:pathology; D008113:Liver Neoplasms / Q000188:drug therapy / Q000473:pathology; D010756:Phosphoric Acids / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000577:Amides; D000970:Antineoplastic Agents; D047309:Flavones; D010756:Phosphoric Acids; C011067:phosphoramidic acid
keywords: Apoptosis; Flavone; G2/M arrest; HepG2; Phosphoramidate