title: Cytotoxicity of chalcone derivatives towards glioblastoma.
abstract: BACKGROUND
  Among seventeen compounds derived from chalcones investigated as potential anticancer drugs towards LN229 glioblastoma cell line, only two were effective.
  
  
  METHODS
  Anticancer activity was investigated by evaluating the cell growth, cell cycle, mitotic index and the cell death.
  
  
  RESULTS
  Two compounds, namely C2 and C12, inhibited cell proliferation associated with a blockade in the G(2)/M phase of the cell cycle and arrested the growth of tumour spheroid mimicking in vivo tumour. C2 blocked cells in the G(2) phase whereas C12 blocked cells in the M phase of the cell cycle. C12 and C2 killed 40% and 95% of the cells respectively using complex mechanisms. The two compounds increased the fluorescence of rhodamine-123 and N-acetylcysteine inhibited their activity, suggesting a role for reactive oxygen species in cell death mediated by these two compounds.
  
  
  CONCLUSIONS
  C2 and C12 are markedly cytostatic and cytolytic to glioblastoma cells and act through different pathways.
authors.affiliation: Laboratoire de Cytologie, Département d'Anatomie et Cytologie Pathologiques, Institut de Biologie et de Pathologie (I.B.P.), Centre Hospitalier Universitaire de Grenoble, BP 217X, 38043 Grenoble cedex 09, France. PChampelovier@chu-grenoble.fr
authors.forename: P
authors.initials: P
authors.lastname: Champelovier
authors.forename: M
authors.initials: M
authors.lastname: Mininno
authors.forename: E
authors.initials: E
authors.lastname: Duchamp
authors.forename: E
authors.initials: E
authors.lastname: Nicolle
authors.forename: V
authors.initials: V
authors.lastname: Curri
authors.forename: A
authors.initials: A
authors.lastname: Boumendjel
authors.forename: J
authors.initials: J
authors.lastname: Boutonnat
mesh_terms: D000111:Acetylcysteine / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002599:Chalcone / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D004354:Drug Screening Assays, Antitumor; D005909:Glioblastoma / Q000473:pathology*; D006801:Humans; D012235:Rhodamines / Q000378:metabolism; D018874:Spheroids, Cellular / Q000187:drug effects / Q000473:pathology; D013329:Structure-Activity Relationship
chemical_list: D012235:Rhodamines; C058319:dihydrorhodamine 123; D002599:Chalcone; D000111:Acetylcysteine