title: Synthesis, characterization, and in vitro anticancer evaluation of novel 2,5-disubstituted 1,3,4-oxadiazole analogue.
abstract: In this series, we have synthesised a new 2,5-disubstituted 1,3,4-oxadiazole in search of potential therapeutics for cancer. The anticancer activities were evaluated on a panel of 60 cell lines by the National Cancer Institute according to its own screening protocol. Out of the 24 compounds, 11 were selected and evaluated via single high dose (10(-5) M). In the next phase, two compounds have been selected for five-dose assay. The compounds 3-(5-benzyl-1,3,4-oxadiazol-2-yl)quinolin-2(1H)-one 18 (NSC-776965) and 3-[5-(2-phenoxymethyl-benzoimidazol-1-ylmethyl)-[1,3,4]oxadiazol-2-yl]-2-p-tolyloxy-quinoline 27 (NSC-776971) showed mean growth percentage of 66.23 and 46.61, respectively, in one-dose assay and their GI50 values ranging between 1.41-15.8 μM and 0.40-14.9 μM, respectively, in 5-dose assay.
authors.affiliation: Department of Pharmaceutical Technology, Noida Institute of Engineering and Technology, Greater Noida, Uttar Pradesh 201306, India.
authors.lastname: Salahuddin
authors.affiliation: Department of Pharmaceutical Technology, Noida Institute of Engineering and Technology, Greater Noida, Uttar Pradesh 201306, India.
authors.forename: Avijit
authors.initials: A
authors.lastname: Mazumder
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), New Delhi 110062, India.
authors.forename: Mohammad
authors.initials: M
authors.lastname: Shaharyar
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000138:chemical synthesis; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006801:Humans; D007928:Lethal Dose 50; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000473:pathology*; D010069:Oxadiazoles / Q000008:administration & dosage* / Q000138:chemical synthesis*; D016896:Treatment Outcome
chemical_list: D000970:Antineoplastic Agents; D010069:Oxadiazoles