Cytotoxic potential of novel 6,7-dimethoxyquinazolines

Herein, we report the synthesis and cytotoxicity of a series of substituted 6,7-dimethoxyquinazoline derivatives. The cytotoxic activity of all synthesized compounds has been evaluated against HCT116p53+/+ and HCT116p53−/− colon cancer cells and a HEY ovarian cancer cell line naturally resistant to cisplatin. Nine of the tested compounds showed significant cytotoxicity in all cell lines at 10 μM. The most promising derivative (7c) showed IC50values of 0.7 and 1.7 μM in the two colon cancer cell lines.

The synthesis and cytotoxicity activity of a series of variously substituted 6,7-dimethoxyquinazoline derivatives is reported. Nine of the tested compounds showed remarkable cytotoxicity in all cell lines.Figure optionsDownload as PowerPoint slideHighlights
► 2/3-Substituted quinazoline derivatives have been synthesized.
► Cytotoxic potential of the synthesized derivatives has been evaluated.
► Flow cytometry analysis has been performed for the most potent derivative.
► The most potent compound (7c) showed IC50 of 1.7 μM on colon cancer cell line.