A straightforward, rapid and efficient one‐pot method was developed for the synthesis of 2,4 ‐diphenyl‐1,2 dihydroquinazoline and their analogues. The reactions were performed with different type of benzylamine and 2‐bromo benzophenone using ammonium acetate and characterized by 1H NMR, 13C NMR and Mass spectroscopic techniques. All the compounds were tested for MDA‐MB‐231, A549 and DU‐145 type of human cancer cell lines. Among the synthesized compounds, 4 j (4‐phenyl‐2‐(3,4,5‐trimethoxyphenyl)‐1,2‐dihydroquinazoline) and 4 e (2‐(3,4‐dichlorophenyl)‐4‐phenyl‐1,2‐dihydroquinazoline) molecules were found to possess good anticancer activity. The binding nature of these molecules was explored through docking studies.