title: Synthesis of new aromatic pyrrolo[2,1-c] [1,4]benzodiazepines and pyrrolo[1,2-a]thieno[3,2-e] [1,4]diazepines as anti-tumoral agents.
abstract: Diazepine analogs of thieno[2,3-b]pyrrolizin-8-ones were synthesized by aromatization of 2-hydroxypyrrolo[1,2-a]thieno[3,2-e][1,4]diazepines. These compounds were evaluated in vitro for their antiproliferative activity against the L1210 leukemia cell line. The activity of these compounds was in the micromolar range, the best result being for the mixture of the isomers 5 and 6 which showed a 0.35 microM IC50 against cell growth.
authors.affiliation: Centre d'Etudes et de Recherche sur le Médicament de Normandie-UFR des Sciences Pharmaceutiques 5, rue Vaubénard 14032 Caen cedex, France.
authors.forename: Vincent
authors.initials: V
authors.lastname: Lisowski
authors.forename: Frédéric
authors.initials: F
authors.lastname: Fabis
authors.forename: Alain
authors.initials: A
authors.lastname: Pierré
authors.forename: Daniel-Henri
authors.initials: DH
authors.lastname: Caignard
authors.forename: Pierre
authors.initials: P
authors.lastname: Renard
authors.forename: Sylvain
authors.initials: S
authors.lastname: Rault
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D001555:Benzene Derivatives / Q000737:chemistry; D001569:Benzodiazepines / Q000737:chemistry* / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D020128:Inhibitory Concentration 50; D007536:Isomerism; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D001555:Benzene Derivatives; D001569:Benzodiazepines