title: Relationship between structure and antiproliferative activity of 1-azaflavanones.
abstract: The synthesis of 19 derivatives of 2-phenyl-3,4-dihydroquinolin-4(1H)-one, as aza analogs of flavanones, was carried out and these compounds were further screened for their antiproliferative activity toward HL60 promyelocytic leukemia cells. In comparison with flavanone the replacement of C-ring ether oxygen atom with a nitrogen atom potentiated activity by more than 100-fold. It was suggested that the aromaticity of the B-ring contributes greatly to the activity of 1-azaflavanones.
authors: Faculty of Science and Engineering, Tokyo Denki University, Hatoyama, Saitama 350-0394, Japan. kawaii@mail.dendai.ac.jp
authors: Satoru
authors: S
authors: Kawaii
authors: Kotaro
authors: K
authors: Endo
authors: Tetsuo
authors: T
authors: Tokiwano
authors: Yuko
authors: Y
authors: Yoshizawa
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D048708:Cell Growth Processes / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D044950:Flavanones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D018922:HL-60 Cells; D006801:Humans; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001372:Aza Compounds; D044950:Flavanones