title: Design, synthesis and anticancer activities of diaryl urea derivatives bearing N-acylhydrazone moiety.
abstract: A new series of diaryl urea derivatives bearing N-acylhydrazone moiety were designed and synthesized. All the target compounds were evaluated for their cytotoxic activities in vitro against human lung adenocarcinoma epithelial cell line (A549), human breast cancer cell line (MDA-MB-231) and human leukemia cell line (HL-60) by standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Several compounds (1a, 1f and 1h) were further evaluated against human embryonic fibroblast, lung-derived cell line (WI38). The pharmacological results indicated that some compounds exhibited promising anticancer activities. In particular, compound 1f showed the most potent cytotoxicity against the tested three cell lines with IC(50) values of 0.41 µM, 0.24 µM and 0.23 µM, respectively.
authors.affiliation: Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, PR China.
authors.forename: Bei
authors.initials: B
authors.lastname: Zhang
authors.forename: Yanfang
authors.initials: Y
authors.lastname: Zhao
authors.forename: Xin
authors.initials: X
authors.lastname: Zhai
authors.forename: Lihui
authors.initials: L
authors.lastname: Wang
authors.forename: Jingyu
authors.initials: J
authors.lastname: Yang
authors.forename: Zehui
authors.initials: Z
authors.lastname: Tan
authors.forename: Ping
authors.initials: P
authors.lastname: Gong
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D015195:Drug Design; D006801:Humans; D006835:Hydrazones / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D021241:Spectrometry, Mass, Electrospray Ionization; D014508:Urea / Q000031:analogs & derivatives* / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D006835:Hydrazones; D014508:Urea