title: Relationship between structure and antiproliferative activity of polymethoxyflavones towards HL60 cells.
abstract: As part of our continuing investigation of polymethoxyflavone (PMF) derivatives as potential anticancer substances, a series of PMF derivatives was synthesized. The synthesized compounds were evaluated for cytotoxicity against the promyelocytic leukemic HL60 cell line, and structure-activity relationship correlations were investigated along with previously isolated PMFs from the peel of king orange (Citrus nobilis). 7,3'-Dimethoxyflavone demonstrated the most potent activity among the synthetic PMFs. Consideration of correlation between the methoxylation pattern and antiproliferative activity revealed the importance of the 3'-methoxyl group and the higher degree of methoxylation on the A-ring moiety of PMFs.
authors.affiliation: Faculty of Science and Engineering, Tokyo Denki University, Hatoyama, Saitama, 350-0394, Japan. kawaii@mail.dendai.ac.jp
authors.forename: Satoru
authors.initials: S
authors.lastname: Kawaii
authors.forename: Tomoyasu
authors.initials: T
authors.lastname: Ikuina
authors.forename: Takeshi
authors.initials: T
authors.lastname: Hikima
authors.forename: Tetsuo
authors.initials: T
authors.lastname: Tokiwano
authors.forename: Yuko
authors.initials: Y
authors.lastname: Yoshizawa
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D048708:Cell Growth Processes / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D047309:Flavones / Q000737:chemistry* / Q000494:pharmacology*; D018922:HL-60 Cells; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D047309:Flavones