title: Synthesis and evaluation of 2,5-di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles as anti-cancer agents.
abstract: A series of 2,5-di(4-aryloylaryloxymethyl)-1,3,4-oxadiazoles 9a-j were obtained via multistep synthesis from hydroxybenzophenones 4a-e. The cytotoxicity of compounds 9a-j was evaluated against human leukemia cell lines (K562 and CEM). The compounds exhibited moderate to good anti-cancer activity with compounds 9b and 9i having a chloro group exhibiting the best activity (IC50 = 10 μM). Compound 9i exhibited activity against both the cell lines and 9b only exhibited activity against CEM. Further, a lactate dehydrogenase (LDH) assay and DNA fragmentation studies of the compounds 9a-j were also performed.
authors.affiliation: Department of Chemistry, Yuvaraja's College Mysore, University of Mysore, Mysore 570 006, India.
authors.forename: H D
authors.initials: HD
authors.lastname: Gurupadaswamy
authors.forename: V
authors.initials: V
authors.lastname: Girish
authors.forename: C V
authors.initials: CV
authors.lastname: Kavitha
authors.forename: Sathees C
authors.initials: SC
authors.lastname: Raghavan
authors.forename: Shaukath Ara
authors.initials: SA
authors.lastname: Khanum
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D053938:DNA Fragmentation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D020128:Inhibitory Concentration 50; D042541:Intracellular Space / Q000187:drug effects / Q000201:enzymology; D020014:K562 Cells; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D008956:Models, Chemical; D015394:Molecular Structure; D010069:Oxadiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013997:Time Factors
chemical_list: D000970:Antineoplastic Agents; D010069:Oxadiazoles; D007770:L-Lactate Dehydrogenase