Novel 1,4-benzodiazepine derivatives with antiproliferative properties on tumor cell lines.
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.
Dourlat
Jennifer
J
Université Paris Descartes, UFR Biomédicale, Laboratoire de Pharmacochimie Moléculaire et Cellulaire, Paris F-75006, France.
Liu
Wang-Qing
WQ
Gresh
Nohad
N
Garbay
Christiane
C
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
D000970:Antineoplastic Agents; D001570:Benzodiazepinones; D001569:Benzodiazepines; C028513:4'-chlorodiazepam; C468549:Bz-423