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Neoplasma Vol.53, p.291-300, 2006 |
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Title: Cytotoxic/antiproliferative effects of new [1,2,4]triazolo[4,3-c] quinazolines in tumor cell lines HeLa and B16 | ||
Author: S., JANTOVA ; S., LETASIOVA ; R., OVADEKOVA ; M., MUCKOVA ; | ||
Abstract: Quinazolines – 1,3-benzodiazines are biological active compounds,
and some of them act as anticancer drugs. We evaluated
cytotoxic/antiproliferative activity of new synthetically prepared
[1,2,4]triazolo[4,3-c]quinazolines using tumor cell
lines HeLa and B16. The in vitro cytotoxic studies of the most
active derivative 3-(5-nitro-2-thienyl)-9-chloro-5-morpholin-
4-yl[1,2,4]triazolo[4,3-c]quinazoline (NTCHMTQ) were complemented
by cell cycle analysis, and determination of
apoptotic DNA fragmentation. Possible direct interaction of
NTCHMTQ with calf thymus DNA was tested by the
DNA-modified screen-printed electrode. Five quinazoline
derivatives tested acted cytotoxically on both tumor cell lines.
The melanoma cells B16 were more sensitive to quinazolines
treatment than HeLa cells. The most effective derivative was
NTCHMTQ which manifested significant in vitro
cytotoxic/antiproliferative effect. NTCHMTQ at micromolar
concetrations induced morphological changes and necrosis of B16
cells. NTCHMTQ at concentrations tested did not cause
changes in cell cycle, did not induce apoptotic cell death in the
B16 cells and did not even behave as a typical intercalating
agent.
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Keywords: [1,2,4]triazolo[4,3-c]quinazolines, cytotoxic/antiproliferative effects, B16 and Hela cells, necrosis, DNA damage | ||
Year: 2006, Volume: 53, Issue: | Page From: 291, Page To: 300 | |
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