Neoplasma Vol.51, p.436-441, 2004
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Title: Cytotoxic and genotoxic effects of some substituted tetrazolo[1,5-
c]quinazolines
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Author: S., JANTOVA
; M., MIKULASOVA
; M., THEISZOVA
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Abstract: Nine substituted tetrazolo[1,5-c]quinazolines have been tested for
cytotoxic effects and structure activity relationship on the
murine cancer cell line B16 and four bacterial strains. The most
cytotoxic activity had non-substituted in the aromatic ring or
substituted by bromo- or chloro- goup, and in the pyrimidine ring
of quinazoline skeleton by phenyl or morpholine group,
respectively. In the bacterium all tested quinazolines had a lower
antibacterial effect than ampicillin. 9-bromo-5-morpholino-
tetrazolo[1,5-c]quinazoline (BMTQ) at the highest concentration
tested (30.0 µmol/l) had an acute cytostatic effect manifested by
the total inhibition of the cell proliferation. Other
concentrations caused a cytotoxicity proportional to the
concentation used. The IC50 values were found to be less than 4
µg/ml, a limit put forward by the National Cancer Institute (NCI)
for clasification of the compound as a potential anticancer drug.
BMTQ induced mutations in a dose-related manner, starting from 10
µg/plate in strains TA100 and TA102. Lesser but significant
increases in revertant colonies were also obtained in strain TA98.
The mutagenity was slighly enhanced by metabolic activation.
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Keywords: Cytotoxicity, genotoxicity, antibacterial activity, quinazoline
derivatives, cancer cell line B16, cell proliferation
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Year: 2004, Volume: 51, Issue: |
Page From: 436, Page To: 441 |
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