title: Growth inhibitory activities of oxyprenylated and non-prenylated naturally occurring phenylpropanoids in cancer cell lines.
abstract: A series of 25 selected oxyprenylated natural phenylpropanoids were synthesized, and their growth inhibitory activities were evaluated in vitro together with 14 other commercially available non-alkylated compounds belonging to the same chemical series. The compounds were tested on six human cancer cell lines using MTT colorimetric assays. The data reveal that of the six chemical groups (G) studied, coumarins (G1), cinnamic and benzoic acids (G2), chalcones (G3), acetophenones (G4), anthraquinones (G5), and cinnamaldehydes and cinnamyl alcohols (G6), G2-related compounds displayed the weakest growth inhibitory activities in vitro, whereas G5-related compounds displayed the highest activities. Quantitative videomicroscopy analyses were then carried out on human U373 glioblastoma cells, which are characterized by various levels of resistance to different pro-apoptotic stimuli. These analyses revealed that compounds 20 (4,2',4'-trihydroxychalcone), and 30 and 31 (two cinnamaldehydes) were cytostatic and able to overcome the intrinsic resistance of U373 cancer cells to pro-apoptotic stimuli.
authors.affiliation: Laboratoire de Toxicologie, Faculté de Pharmacie, Université Libre de Bruxelles (ULB), Brussels, Belgium.
authors.forename: Céline
authors.initials: C
authors.lastname: Bruyère
authors.forename: Salvatore
authors.initials: S
authors.lastname: Genovese
authors.forename: Benjamin
authors.initials: B
authors.lastname: Lallemand
authors.forename: Alexandra
authors.initials: A
authors.lastname: Ionescu-Motatu
authors.forename: Massimo
authors.initials: M
authors.lastname: Curini
authors.forename: Robert
authors.initials: R
authors.lastname: Kiss
authors.forename: Francesco
authors.initials: F
authors.lastname: Epifano
mesh_terms: D000098:Acetophenones / Q000737:chemistry / Q000494:pharmacology; D000171:Acrolein / Q000031:analogs & derivatives / Q000737:chemistry / Q000494:pharmacology; D000880:Anthraquinones / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017209:Apoptosis; D001565:Benzoates / Q000737:chemistry / Q000494:pharmacology; D001688:Biological Products / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology; D002934:Cinnamates / Q000737:chemistry / Q000494:pharmacology; D003374:Coumarins / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D054876:Prenylation; D020005:Propanols / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000098:Acetophenones; D000880:Anthraquinones; D000970:Antineoplastic Agents; D001565:Benzoates; D001688:Biological Products; D047188:Chalcones; D002934:Cinnamates; D003374:Coumarins; D020005:Propanols; C029010:cinnamic acid; D000171:Acrolein; C012843:cinnamaldehyde; C020722:cinnamyl alcohol