title: Synthesis and evaluation of 2-[2-(phenylthiomethyl)-1H-benzo[d] imidazol-1-yl)acetohydrazide derivatives as antitumor agents.
abstract: A novel class of acetylhydrazone derivatives (5a-x) containing 2-(phenylthiomethyl)-1H-benzo-[d]-imidazole moieties are synthesizer, and their antitumor activities against A549, HCT116, HepG2, PC-9, and A375 were determined by the MTT assay. Among them are N-(2,4-dihydroxybenzylidene)-2-(2-(phenylthiomethyl)-1H-benzo[d]-imidazol-1-yl)acetohydrazide (5a) and N-(5-bromo-2-hydroxy-benzylidene)-2-(2-(phenylthiomethyl)-1H-benzo[d]-imidazol-1-yl)acetohydrazide (5d) which displayed excellent cancer inhibitory activity against the tested cancer cells (IC(50) 4-17 μM), compared with 5-FU and SU11248. The others have moderate to weak inhibitory activity against the tested cancer cell lines.
authors.affiliation: Department of Pharmaceutical and Bioengineering, School of Chemical Engineering, Sichuan University, Chengdu, Sichuan 610065, PR China.
authors.forename: Ting
authors.initials: T
authors.lastname: Liu
authors.forename: Changyan
authors.initials: C
authors.lastname: Sun
authors.forename: Xiumei
authors.initials: X
authors.lastname: Xing
authors.forename: Lingling
authors.initials: L
authors.lastname: Jing
authors.forename: Rui
authors.initials: R
authors.lastname: Tan
authors.forename: Youfu
authors.initials: Y
authors.lastname: Luo
authors.forename: Wencai
authors.initials: W
authors.lastname: Huang
authors.forename: Hang
authors.initials: H
authors.lastname: Song
authors.forename: Zicheng
authors.initials: Z
authors.lastname: Li
authors.forename: Yinglan
authors.initials: Y
authors.lastname: Zhao
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D016923:Cell Death / Q000187:drug effects; D045744:Cell Line, Tumor; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology; D007093:Imidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D006835:Hydrazones; D007093:Imidazoles