title: Antimitotic and antiproliferative activities of chalcones: forward structure-activity relationship.
abstract: A series of 59 chalcones was prepared and evaluated for the antimitotic effect against K562 leukemia cells. The most active chalcones were evaluated for their antiproliferative activity against a panel of 11 human and murine cell cancer lines. We found that three chalcones were of great interest as potential antimitotic drugs. In vivo safety studies conducted on one of the most active chalcones revealed that the compound was safe, allowing further in vivo antitumor evaluation.
authors.affiliation: Département de Pharmacochimie Moléculaire, UMR 5063, ICMG-FR 2607-Université Joseph Fourier Grenoble I, 470 rue de la Chimie, 38240 St Martin d'Hères, France. ahcene.boumendjel@ujf-grenoble.fr
authors.forename: Ahcène
authors.initials: A
authors.lastname: Boumendjel
authors.forename: Julien
authors.initials: J
authors.lastname: Boccard
authors.forename: Pierre-Alain
authors.initials: PA
authors.lastname: Carrupt
authors.forename: Edwige
authors.initials: E
authors.lastname: Nicolle
authors.forename: Madeleine
authors.initials: M
authors.lastname: Blanc
authors.forename: Annabelle
authors.initials: A
authors.lastname: Geze
authors.forename: Luc
authors.initials: L
authors.lastname: Choisnard
authors.forename: Denis
authors.initials: D
authors.lastname: Wouessidjewe
authors.forename: Eva-Laure
authors.initials: EL
authors.lastname: Matera
authors.forename: Charles
authors.initials: C
authors.lastname: Dumontet
mesh_terms: D000818:Animals; D050256:Antimitotic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D047188:Chalcones / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D004354:Drug Screening Assays, Antitumor; D064420:Drug-Related Side Effects and Adverse Reactions; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D015996:Survival Rate
chemical_list: D050256:Antimitotic Agents; D000970:Antineoplastic Agents; D047188:Chalcones