Abstract

A series of new 2, 4-disubstituted quinazolines were synthesized by an analog design approach. The synthesis of title compounds (3a–f, 4a–c, 5a–c, and 6a–c) was achieved from the corresponding key intermediates 2-(pyridin- 3-yl) quinazolin-4(3H)-one(2a), 2-(pyridin-3-yl) quinazolin-4(3H)-one (2b) and 2-(pyrazin-2-yl)quinazolin-4(3H)- one (2c) with appropriate amines. The synthesized compounds were characterized by the spectral studies. All the synthesized compounds were evaluated for in vitro anticancer activity employing 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide assay against human adenocarcinoma (HT-29), breast cancer (MDA-231), and Ehrlich ascites carcinoma cell lines. Among the tested compounds, 5a has a significant anticancer activity (5.33 μM/ml) against the human adenocarcinoma cell line. Other compounds have shown a moderate anticancer activity against the tested cell lines.

Key words: 2, 4-disubstituted quinazolines, anticancer activity, MTT assay and human adenocarcinoma cells