title: Synthesis and antiproliferative assay of 1,3,4-oxadiazole and 1,2,4-triazole derivatives in cancer cells.
abstract: A series of new 1,3,4-oxadiazole and 1,2,4-triazole derivatives were synthesized. The structures were confirmed by IR, (1)H-NMR, and MS. The compounds were evaluated for their antiproliferative activity against K562 (human erythromyeloblastoid leukemia cell line), MDA-MB-231 (human breast adenocarcinoma cell line), HT29 (human colon adenocarcinoma grade II cell line) and HepG2 (human hepatocellular liver carcinoma cell line) in vitro. The result showed that 7 compounds displayed inhibitory activities against K562 with the inhibition rate more than 50%. Especially, compound 5f exhibited the most potent activity against K562 with 85% inhibition ratio and could be used as lead compound to search new 1,3,4-oxadiazole derivatives as antiproliferative agent.
authors.affiliation: Department of Medicinal Chemistry, School of Pharmacy, Nanchang University, Nanchang, Jiangxi, China.
authors.forename: Guogang
authors.initials: G
authors.lastname: Tu
authors.forename: Yugang
authors.initials: Y
authors.lastname: Yan
authors.forename: Xueying
authors.initials: X
authors.lastname: Chen
authors.forename: Qiaoli
authors.initials: Q
authors.lastname: Lv
authors.forename: Jiaqi
authors.initials: J
authors.lastname: Wang
authors.forename: Shaohua
authors.initials: S
authors.lastname: Li
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D019073:HT29 Cells; D056945:Hep G2 Cells; D006801:Humans; D020014:K562 Cells; D010069:Oxadiazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D010069:Oxadiazoles; D014230:Triazoles; C583463:1,3,4-oxadiazole; C045575:1,2,4-triazole