title: Design, synthesis and pharmacological evaluation of new anticancer fused pentacycles.
abstract: The quinoline chromophore has long formed the basis for the clinical development of novel antitumour agents. Camptothecin derivatives have already proved their clinical efficacy and compounds such as ascididemin (pyridoacridine family), DHDMC (protoberberine family) have a very promising future. During our search for new cytotoxic molecules, we have designed compounds based on the benzo[c]pyrido[2,3,4-kl]acridine skeleton which combines the structural features of ascididemin and DHDMC. Corresponding compounds were synthesized and evaluated for their cytotoxic activity against human prostatic PC-3 cell lines. Some have shown promising biological activity in inhibiting the growth of cell lines which are resistant to camptothecin.
authors.affiliation: Institut de Chimie Pharmaceutique Albert Lespagnol, EA 2692, Université de Lille 2, BP 83, 59006 Lille, France.
authors.forename: Sarah
authors.initials: S
authors.lastname: Chackal
authors.forename: Raymond
authors.initials: R
authors.lastname: Houssin
authors.forename: Nicole
authors.initials: N
authors.lastname: Pommery
authors.forename: Jean-Pierre
authors.initials: JP
authors.lastname: Henichart
mesh_terms: D000166:Acridines / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002455:Cell Division / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D008297:Male; D015394:Molecular Structure; D011471:Prostatic Neoplasms / Q000473:pathology; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000166:Acridines; D000970:Antineoplastic Agents; D011725:Pyridines