SYNTHESIS AND CYTOTOXIC ACTIVITY OF N-PHENYLATED DERIVATIVES OF 5- HALOPYRIMIDINE-2,4-DIONE

Abstract

The presented research project demonstrates new synthetic strategy for providing 5-
halopyrimidine-2,4-dione derivatives comprising promising cytotoxicity. This study was carried out to
explore the prospective future directions on the development of more effective yet specific 5-
halopyrimidine-2,4-dione analogues effectively showing anticancer activity. Pyrimidine-2,4-dione is
considered as privileged structures in drug discovery owing to marked medicinal potential and
synthetic accessibility. As a result, a variety-oriented synthesis of multifaceted organic molecules from
simple and readily available substrate has been carried out that has resulted in the derivatization of 5-
halopyrimidine-2,4-dione predominantly giving N1 substituted compounds. In addition, microwaveassisted solvent free conditions using solid support has proved to be of dynamic importance in term of
energy efficacy and designing of an ecofriendly synthetic route with significantly reduced reaction
time. Newly formed N-alkylated derivatives show greater anticancer activity determined by He La cell
line.