Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives

Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared and their cytotoxic activities were tested in five human tumor cell lines. Some compounds (5e, 5k, 5t, 6c and 6f) showed relatively high cytotoxic activity. Especially, compound 6c showed the most cytotoxicity against all cell lines tested among the synthesized derivatives, and the inhibitory activity of 6c against HeLa cell was higher than that of adriamycin. The putative mechanism of antitumor action in apoptotic cell death was cell cycle arrest in the G0/G1 phase by compounds 5k, 5v, 5m, 6c, and 6f in HeLa cells. These compounds showed relatively high cytotoxicity in this cell type.

Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared and their cytotoxicity against five human tumor cell lines was tested. 6c showed the most cytotoxicity against all cell lines among synthesized compounds.Figure optionsDownload as PowerPoint slideHighlights
► Thirty 2-phenylquinazolin-4(3H)-one derivatives were prepared.
► And their cytotoxic activities were tested in five human tumor cell lines.
► Compounds 5e, 5k, 5t, 6c and 6f showed relatively high cytotoxic activity.
► The most active 6c showed higher activity against Hela than that of adriamycin.
► The putative mechanism of action was cell cycle arrest in the G0/G1 phase.