title: Cytotoxic activity of 5-benzoylimidazole and related compounds against human oral tumor cell lines.
abstract: A total of 24 benzoylimidazoles and structurally-related compounds were investigated for their cytotoxic activity against oral tumor cells and normal gingival fibroblast. Compound 23 (5-(2-hydroxylbenzoyl)-2-phenylimidazole) showed the highest cytotoxic activity against both human oral tumor cell lines (human squamous cell carcinoma HSC-2, human salivary gland tumor HSG) and normal human gingival fibroblast (HGF). Compounds 7 (2-(2-hydroxybenzoyl)benz imidazo[2,1-b]thiazole), 14 (1,3-diethyl-5-(2-hydroxybenzoyl)-4-imidazoline-2-thione) and 18 (5-(2-hydroxy-4-methoxybenzoyl)-3-methyl-2-methylimino-4-thiazoline) showed slightly lower cytotoxic activity, but higher tumor-specific cytotoxic action. The cytotoxic activity of compound 23 was significantly reduced by CuCl2, but not by CoCl2, FeCl3, or by antioxidants (N-acetyl-L-cysteine, sodium ascorbate, catalase). Compound 23 did not show any detectable oxidation potential (determined by NO monitor). Agarose gel electrophoresis demonstrated that compound 23 induced DNA fragmentation in human promyelocytic leukemia cells HL-60, but not in HSG cells. These data suggested that the response to compound 23 might be different from cell to cell.
authors.affiliation: Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350-0295, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Terasawa
authors.forename: Y
authors.initials: Y
authors.lastname: Sugita
authors.forename: I
authors.initials: I
authors.lastname: Yokoe
authors.forename: S
authors.initials: S
authors.lastname: Fujisawa
authors.forename: H
authors.initials: H
authors.lastname: Sakagami
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D000975:Antioxidants / Q000494:pharmacology; D002294:Carcinoma, Squamous Cell; D053938:DNA Fragmentation; D004354:Drug Screening Assays, Antitumor; D018922:HL-60 Cells; D006801:Humans; D007093:Imidazoles / Q000737:chemistry / Q000494:pharmacology*; D008670:Metals; D015394:Molecular Structure; D009062:Mouth Neoplasms; D012468:Salivary Gland Neoplasms; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D000975:Antioxidants; D007093:Imidazoles; D008670:Metals; C052702:N-benzoylimidazole