Synthesis and Cytotoxic Activity of 5-Benzoylhexahydropyrimidine Derivatives

The reaction of ethyl benzoylacetate with formaldehyde and natural amino acid ester hydrochlorides in acetate buffer (AcONa/AcOH, pH 4.0) at room temperature afforded 41–61% of new 5-benzoylhexahydropyrimidine derivatives. The synthesized compounds were evaluated for their in vitro cytotoxic activity against normal (HEK293) and tumor cell lines (Jurkat, HepG2). T-Lymphoblastic leukemia Jurkat cells turned out to be most sensitive to the examined hexahydropyrimidine derivatives. Ethyl 5-benzoyl-1,3-bis[2-ethoxy-1-(4-hydroxybenzyl)-2-oxoethyl]hexahydropyrimidine-5-carboxylate showed the highest cytotoxic activity against all tested cell lines.