title: Novel 1,4-benzodiazepine derivatives with antiproliferative properties on tumor cell lines.
abstract: Novel 1,4-benzodiazepine compounds were synthesized and evaluated for their ability to inhibit the proliferation of tumor cells. Some compounds revealed activities in the micromolar range and were more efficient than reference compound Ro 5-4864. Preliminary SAR helped to identify critical motifs for antiproliferative activity and led to the discovery of a compound selective for a melanoma cell line, known for its resistance to chemotherapy.
authors.affiliation: Université Paris Descartes, UFR Biomédicale, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, Paris F-75006, France.
authors.forename: Jennifer
authors.initials: J
authors.lastname: Dourlat
authors.forename: Wang-Qing
authors.initials: WQ
authors.lastname: Liu
authors.forename: Nohad
authors.initials: N
authors.lastname: Gresh
authors.forename: Christiane
authors.initials: C
authors.lastname: Garbay
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology; D001570:Benzodiazepinones / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D008545:Melanoma / Q000188:drug therapy; D008956:Models, Chemical; D008968:Molecular Conformation
chemical_list: D000970:Antineoplastic Agents; D001570:Benzodiazepinones; D001569:Benzodiazepines; C028513:4'-chlorodiazepam; C468549:Bz-423