title: Solution-phase parallel synthesis and screening of anti-tumor activities from fenbufen and ethacrynic acid libraries.
abstract: The derivatives with fenbufen and ethacrynic acid core compounds was synthesized through a facial preparation of 1-amino-4-azidobutane. The subsequent coupling with 102 members of carboxylic acids afforded amide products. The in situ screening using colorimetric assay with 3-(4.5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide showed that fenbufen but not ethacrynic acid butyl amide members displayed the cytotoxicities to tumor cells substantially, including two human cell lines (MCF7 and A549) and two murine cell lines (C26 and TRAMP-C1). Three fenbufen analogs were found to have a good anti-tumor activity comparable to cisplatin.
authors.affiliation: Department of Biomedical Engineering and Environmental Sciences, National Tsing-Hua University, Hsinchu, Taiwan.
authors.forename: Yuan-Hsiao
authors.initials: YH
authors.lastname: Su
authors.forename: Li-Wu
authors.initials: LW
authors.lastname: Chiang
authors.forename: Kee-Ching
authors.initials: KC
authors.lastname: Jeng
authors.forename: Ho-Lien
authors.initials: HL
authors.lastname: Huang
authors.forename: Jenn-Tzong
authors.initials: JT
authors.lastname: Chen
authors.forename: Wuu-Jyh
authors.initials: WJ
authors.lastname: Lin
authors.forename: Chia-Wen
authors.initials: CW
authors.lastname: Huang
authors.forename: Chung-Shan
authors.initials: CS
authors.lastname: Yu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D004976:Ethacrynic Acid / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D051379:Mice; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy; D010654:Phenylbutyrates / Q000737:chemistry* / Q000494:pharmacology; D054852:Small Molecule Libraries
chemical_list: D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D010654:Phenylbutyrates; D054852:Small Molecule Libraries; C010725:fenbufen; D004976:Ethacrynic Acid