Abstract
Objectives: The aim of the present research was to synthesise several novel fluorinated quinazoline-sulphonamide derivatives and to evaluate their in vitro cytotoxic activity.
Methods: Eight compounds were synthesised. The compounds' anticancer activities were determined through the [3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyltetrazolium bromide] (MTT) assay using a three-cell-line panel consisting of National Cancer Institute (NCI) lung cancer cells, Michigan Cancer Foundation-7 (MCF-7) breast cancer cells, and Human Embryonic Kidney-293 (HEK-293) normal kidney cell. The values of C log P correlations were determined to interpret the results.
Results: One compound exhibited significant anticancer activity with low toxicity compared with the methotrexate as the reference drug. The biological screening showed good to moderate anticancer activity for the title compounds compared with the reference drug. The reference drug exhibited an IC50 value of 2.4 mu M, whereas compound 9, which was identified as the most active compound, exhibited an IC50 value of 2.51 mu M on the NCI cell line. The other compounds showed IC50 values that ranged from 2.89 to 46.34 mu M on the three cell lines. The newly synthesized compounds had lower toxicity on the normal cell line than did methotrexate.
Conclusions: The newly synthesized compounds may provide a valuable template for future design and optimization to produce analogues that act as more active anticancer agents.