title: Synthesis and cytotoxic evaluation of novel dimethyl [1,1'-biphenyl]-2,2'-dicarboxylates bearing 1,3,4-thiadiazole moieties.
abstract: In search of novel anticancer agents, two series of dimethyl [1,1'-biphenyl]-2,2'-dicarboxylate derivatives, 8a-8k and 9a-9k, containing both methylenedioxy and 1,3,4-thiadiazole moieties were designed and synthesized. Cytotoxicity of these compounds was evaluated in vitro against five human tumor cell lines, i.e., HepG2, KB, A549, K562, and MCF-7. The results indicated that 8h, 8j, 8k, 9d, 9g, 9h, 9j, and 9k showed notable anticancer activities comparable to or stronger than that of 5-fluorouracil, a canonical anticancer drug. Structure-activity relationships were also discussed based on the experimental data obtained.
authors.affiliation: Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, P. R. China.
authors.forename: Xiang-Wen
authors.initials: XW
authors.lastname: Kong
authors.forename: Yi-Hua
authors.initials: YH
authors.lastname: Zhang
authors.forename: Tao
authors.initials: T
authors.lastname: Wang
authors.forename: Yi-Sheng
authors.initials: YS
authors.lastname: Lai
authors.forename: Si-Xun
authors.initials: SX
authors.lastname: Peng
mesh_terms: D001713:Biphenyl Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D008745:Methylation; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013830:Thiadiazoles / Q000737:chemistry*
chemical_list: D001713:Biphenyl Compounds; D013830:Thiadiazoles; C039204:diphenic acid