title: Cytotoxicity and detection of damage to DNA by 3-(5-nitro-2-thienyl)-9-chloro-5-morpholin-4-yl[1,2,4]triazolo[4,3-c] quinazoline on human cancer cell line HeLa.
abstract: Quinazolines - 1,3-benzodiazines are biological active compounds, which are used in the phamaceutical industry, in agriculture and in the medicine. As documented in the literature, many derivatives demonstrated anticancer activity and they act as multitarget agents. 3-(5-Nitro-2-thienyl)-9-chloro-5-morpholin-4-yl[1,2,4]triazolo[4,3-c] quinazoline (NTCHMTQ) - a new synthetically prepared quinazoline derivative was the most effective derivative in our primary cytotoxic screening. In this study, we evaluated cytotoxic/antiproliferative activity of NTCHMTQ using human tumor cell line HeLa. Possible interaction of 3-(5-nitro-2-thienyl)-9-chloro-5-morpholin-4-yl[1,2,4]triazolo[4,3-c] quinazoline with calf thymus DNA was tested by the DNA - modified screen - printed electrode. Quinazoline derivative acted cytotoxically on tumor cell line HeLa. The IC(100) value was 10 microg/ml. The IC(50) values was found to be less than 4 microg/ml, a limit put forward by the National Cancer Institute (NCI) for classification of he compound as a potential anticancer drug. Quinazoline at micromolar concentrations induced morphological changes and necrosis of HeLa cells. Using the DNA based electrochemical biosensor, we have not found damage to DNA under in vitro conditions at an incubation of the biosensor in mixture with quinazoline.
authors.affiliation: Department of Analytical Chemistry, Slovak University of Technology, Radlinského 9, Bratislava, Slovak Republic. renata.ovadekova@stuba.sk
authors.forename: Renáta
authors.initials: R
authors.lastname: Ovádeková
authors.forename: Sona
authors.initials: S
authors.lastname: Jantová
authors.forename: Marica
authors.initials: M
authors.lastname: Theiszová
authors.forename: Ján
authors.initials: J
authors.lastname: Labuda
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D002417:Cattle; D004249:DNA Damage / Q000187:drug effects*; D004354:Drug Screening Assays, Antitumor; D006367:HeLa Cells; D006801:Humans; D011799:Quinazolines / Q000494:pharmacology*; D014230:Triazoles / Q000494:pharmacology*
chemical_list: C516744:3-(5-nitro-2-thienyl)-9-chloro-5-morpholin-4-yl(1,2,4)triazolo(4,3-c)quinazoline; D000970:Antineoplastic Agents; D011799:Quinazolines; D014230:Triazoles