title: Antineoplastic activity of benzimidazo[1,2-b]-isoquinolines, indolo[2,3-b]quinolines, and pyridocarbazoles.
abstract: Substituted pyrido[3,4-b]carbazoles, pyrido[2,3-b]carbazoles, indolo[2,3-b]quinolines, and benzimidazo[1,2-b]-isoquinolines were synthesized and evaluated for biological activity. Several methylated derivatives of these heterocyclic compounds had similar activity to ellipticine as mammalian topoisomerase II inhibitors. Methylated derivatives of these heterocyclic compounds were also highly active in vitro, inhibiting the growth of several human tumor cell lines. These data demonstrate that the antineoplastic activity associated with ellipticine can be retained within a wide variety of analogous heterocyclics.
authors.affiliation: Department of Pharmaceutical Chemistry, College of Pharmacy, Rutgers, State University of New Jersey, Piscataway 08855.
authors.forename: R L
authors.initials: RL
authors.lastname: Weinkauf
authors.forename: A Y
authors.initials: AY
authors.lastname: Chen
authors.forename: C
authors.initials: C
authors.lastname: Yu
authors.forename: L
authors.initials: L
authors.lastname: Liu
authors.forename: L
authors.initials: L
authors.lastname: Barrows
authors.forename: E J
authors.initials: EJ
authors.lastname: LaVoie
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002227:Carbazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D004611:Ellipticines / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors; D014407:Tumor Cells, Cultured / Q000187:drug effects
chemical_list: D000970:Antineoplastic Agents; D002227:Carbazoles; D004611:Ellipticines; D007546:Isoquinolines; D011804:Quinolines; D059005:Topoisomerase II Inhibitors; C034192:ellipticine