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.
Highlights
Quinazoline derivatives are used in the pharmaceutical industry, in medicine and in agriculture because of their antimicrobial, anti-inflammatory, diuretic, anticonvulsant, antiallergic, antihypertensive, antiparkinsonian effects and other properties1-4.As documented in the literature, many derivatives act as anticancer active compounds and they act as multitarget agents
We investigated the cytotoxic effect of 3-(5-nitro-2-thienyl)-9-chloro-5-morpholin-4-yl[1,2,4]triazolo[4,3-c] quinazoline on further cancer cell line HeLa and the electrochemical interaction of quinazoline with dsDNA at carbon paste electrode
Quinazoline prepared by Špirková et al.10,11 was dissolved in dimethyl sulfoxide (DMSO)
Summary
Quinazoline derivatives are used in the pharmaceutical industry, in medicine and in agriculture because of their antimicrobial, anti-inflammatory, diuretic, anticonvulsant, antiallergic, antihypertensive, antiparkinsonian effects and other properties1-4.As documented in the literature, many derivatives act as anticancer active compounds 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) is new synthetically prepared derivative, which in our previous study showed cytotoxic effects on cancer cell line B16. We investigated the cytotoxic effect of 3-(5-nitro-2-thienyl)-9-chloro-5-morpholin-4-yl[1,2,4]triazolo[4,3-c] quinazoline on further cancer cell line HeLa and the electrochemical interaction of quinazoline with dsDNA at carbon paste electrode.
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