title: Novel imidazo[1,2-a]naphthyridinic systems (part 1): synthesis, antiproliferative and DNA-intercalating activities.
abstract: Novel imidazo[1,2-a]naphthyridinic systems 6a-15a and 6b-15b were obtained from Friedländer's reaction in imidazo[1,2-a]pyridine series. Most of the compounds were evaluated for their antitumor activity in the NCIs in vitro human tumor cell line screening panel. Among them, pentacyclic derivatives 13b and 14a exhibited in vitro activity comparable to anticancer agent such as amsacrine. Their mechanism of cytotoxicity action was unrelated to poisoning or inhibiting abilities against topo1. On the contrary, we highlighted a direct intercalation of the drugs into DNA by electrophoresis on agarose gel.
authors.affiliation: Univ Clermont 1, UFR Pharmacie, Clermont-Ferrand F-63001, France.
authors.forename: Mounir
authors.initials: M
authors.lastname: Andaloussi
authors.forename: Emmanuel
authors.initials: E
authors.lastname: Moreau
authors.forename: Nicolas
authors.initials: N
authors.lastname: Masurier
authors.forename: Jacques
authors.initials: J
authors.lastname: Lacroix
authors.forename: René C
authors.initials: RC
authors.lastname: Gaudreault
authors.forename: Jean-Michel
authors.initials: JM
authors.lastname: Chezal
authors.forename: Anas
authors.initials: A
authors.lastname: El Laghdach
authors.forename: Damien
authors.initials: D
authors.lastname: Canitrot
authors.forename: Eric
authors.initials: E
authors.lastname: Debiton
authors.forename: Jean-Claude
authors.initials: JC
authors.lastname: Teulade
authors.forename: Olivier
authors.initials: O
authors.lastname: Chavignon
mesh_terms: D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004247:DNA / Q000737:chemistry*; D006801:Humans; D007093:Imidazoles / Q000737:chemistry*; D007364:Intercalating Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D007093:Imidazoles; D007364:Intercalating Agents; D009287:Naphthyridines; C029899:imidazole; D004247:DNA