title: Synthesis and in vitro antitumor activity of ring C and D-substituted phenanthrolin-7-one derivatives, analogues of the marine pyridoacridine alkaloids ascididemin and meridine.
abstract: A series of cycle C and D-substituted phenanthrolin-7-ones, analogues of the marine pyridoacridines meridine and ascididemin have been synthesized on the basis of Diels-Alder reactions involving quinoline-5,8-dione and 2- (or un)-substituted-N,N-dimethylhydrazones. All the compounds were evaluated for in vitro cytotoxic activity against 12 distinct human cancer cell lines. They all exhibit cytotoxic activity with IC(50) values at least of micromolar order.
authors.affiliation: Centre de Phytopharmacie, FRE-CNRS 2605, Université de Perpignan, 52 Avenue Paul Alduy, 66860 Perpignan Cedex, France. delfourn@chimie.ups-tlse.fr
authors.forename: Evelyne
authors.initials: E
authors.lastname: Delfourne
authors.forename: Robert
authors.initials: R
authors.lastname: Kiss
authors.forename: Laurent
authors.initials: L
authors.lastname: Le Corre
authors.forename: Frederic
authors.initials: F
authors.lastname: Dujols
authors.forename: Jean
authors.initials: J
authors.lastname: Bastide
authors.forename: Françoise
authors.initials: F
authors.lastname: Collignon
authors.forename: Brigitte
authors.initials: B
authors.lastname: Lesur
authors.forename: Armand
authors.initials: A
authors.lastname: Frydman
authors.forename: Francis
authors.initials: F
authors.lastname: Darro
mesh_terms: D000166:Acridines / Q000737:chemistry; D000470:Alkaloids / Q000138:chemical synthesis* / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D045744:Cell Line, Tumor; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006576:Heterocyclic Compounds, 4 or More Rings / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D015394:Molecular Structure; D010618:Phenanthrolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011804:Quinolines / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000166:Acridines; D000470:Alkaloids; D000970:Antineoplastic Agents; D006576:Heterocyclic Compounds, 4 or More Rings; D010618:Phenanthrolines; D011804:Quinolines; C475900:pyridoacridine; C079196:meridine; C412046:ascididemin