title: Epoxide-containing side chains enhance antiproliferative activity of paullones.
abstract: The introduction of side chains bearing epoxide motifs into the molecular scaffold of kenpaullone and 9-trifluoromethylpaullone led to improved antiproliferative activity of the novel derivatives for human tumor cell lines. The syntheses were accomplished applying Stille coupling for the introduction of unsaturated side chains into the 2-position of the paullones and subsequently employing a hydrogen peroxide/nitrile mixture for the epoxidation of C,C-double bonds.
authors.affiliation: Institut für Pharmazie, Universität Hamburg, Bundesstrasse 45, D-20146 Hamburg, Germany.
authors.forename: Xu
authors.initials: X
authors.lastname: Xie
authors.forename: Thomas
authors.initials: T
authors.lastname: Lemcke
authors.forename: Rick
authors.initials: R
authors.lastname: Gussio
authors.forename: Daniel W
authors.initials: DW
authors.lastname: Zaharevitz
authors.forename: Maryse
authors.initials: M
authors.lastname: Leost
authors.forename: Laurent
authors.initials: L
authors.lastname: Meijer
authors.forename: Conrad
authors.initials: C
authors.lastname: Kunick
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001552:Benzazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D004354:Drug Screening Assays, Antitumor; D004852:Epoxy Compounds / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D001552:Benzazepines; D004852:Epoxy Compounds; D007211:Indoles; C119620:kenpaullone