Synthesis and in vitro antitumor activity of phenanthrolin-7-one derivatives, analogues of the marine pyridoacridine alkaloids ascididemin and meridine: structure-activity relationship.
A series of substituted pyrido[4,3,2-de][1,7] or [1,10]-phenanthrolin-7-ones, analogues of the marine pyridoacridines meridine and ascididemin, have been synthesized on the basis of Diels-Alder reactions involving different quinoline-5,8-diones and N,N-aldehyde-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.
Delfourne
Evelyne
E
Centre de Phytopharmacie, UMR-CNRS 5054, Université de Perpignan, 52 Avenue de Villeneuve, 66860 Perpignan Cedex, France. delfourn@univ.perp.fr
Kiss
Robert
R
Le Corre
Laurent
L
Dujols
Frederic
F
Bastide
Jean
J
Collignon
Françoise
F
Lesur
Brigitte
B
Frydman
Armand
A
Darro
Francis
F
D000470:Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006835:Hydrazones / Q000737:chemistry; D010618:Phenanthrolines; D011804:Quinolines / Q000737:chemistry; D013329:Structure-Activity Relationship
D000470:Alkaloids; D000970:Antineoplastic Agents; D006835:Hydrazones; D010618:Phenanthrolines; D011804:Quinolines; C079196:meridine; C412046:ascididemin