Prediction of antitumor activity of 3-substituted quinazolinone derivatives synthesized in one-pot method catalyzed by bi(otf)₃

A series of 3-substituted guinazolinone derivatives have been synthesized in good to excellent yields and high selectivity by one-pot reaction using anthranilic acid, amine and orthoester in ethanol under mild conditions, respectively. The reaction was efficiently promoted by Bi(OTf)3 and the catalyst could be recovered easily after the reactions and reused without evident loss of reactivity. Docking studies have shown that the tested molecules have an affinity for anticancer targets. The data obtained can be used in planning experimental screening for antitumor activity.