title: Synthesis, anticancer activity and mitochondrial mediated apoptosis inducing ability of 2,5-diaryloxadiazole-pyrrolobenzodiazepine conjugates.
abstract: A series of 2,5-diaryloxadiazole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates have been prepared and evaluated for their anticancer activity. These conjugates have shown promising activity with GI50 values ranging from <0.1 to 0.29 microM. It is observed that some of these conjugates particularly 4a, 4d, 4i and 4l exhibit significant anticancer activity. Some detailed biological assays relating to the cell cycle aspects associated to Bax and caspases have been examined with a view to understand the mechanism of action of these conjugates.
authors: Chemical Biology Laboratory, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India. ahmedkamal@iict.res.in
authors: Ahmed
authors: A
authors: Kamal
authors: D
authors: D
authors: Dastagiri
authors: M Janaki
authors: MJ
authors: Ramaiah
authors: E Vijaya
authors: EV
authors: Bharathi
authors: J Surendranadha
authors: JS
authors: Reddy
authors: G
authors: G
authors: Balakishan
authors: Pranjal
authors: P
authors: Sarma
authors: S N C V L
authors: SN
authors: Pushpavalli
authors: Manika
authors: M
authors: Pal-Bhadra
authors: Aarti
authors: A
authors: Juvekar
authors: Subrata
authors: S
authors: Sen
authors: Surekha
authors: S
authors: Zingde
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use; D017209:Apoptosis; D001569:Benzodiazepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000627:therapeutic use; D020169:Caspases / Q000378:metabolism; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D051357:Cyclin-Dependent Kinase 2 / Q000378:metabolism; D006801:Humans; D008297:Male; D051379:Mice; D016688:Mice, Inbred NOD; D008928:Mitochondria / Q000187:drug effects*; D009369:Neoplasms / Q000188:drug therapy; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000737:chemistry*; D016159:Tumor Suppressor Protein p53 / Q000378:metabolism; D023041:Xenograft Model Antitumor Assays; D051028:bcl-2-Associated X Protein / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D010069:Oxadiazoles; D016159:Tumor Suppressor Protein p53; D051028:bcl-2-Associated X Protein; D001569:Benzodiazepines; D051357:Cyclin-Dependent Kinase 2; D020169:Caspases