Home Neoplasma 2004 Neoplasma Vol.51, p.436-441, 2004

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Founded: 1954
ISSN 0028-2685
ISSN 1338-4317 (online)

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Neoplasma Vol.51, p.436-441, 2004

Title: Cytotoxic and genotoxic effects of some substituted tetrazolo[1,5- c]quinazolines

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.

Keywords: Cytotoxicity, genotoxicity, antibacterial activity, quinazoline derivatives, cancer cell line B16, cell proliferation
Year: 2004, Volume: 51, Issue: Page From: 436, Page To: 441

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