No abstract

With the aim of obtaining potential antitumor candidates with more efficiency and more economic value. 40 2,4,6-trisubstituted pyrimidine derivatives bearing chalcone moiety were synthesized via cyclization, chlorination, substitution with benzoylacetate and ethylacetoacetate as the starting materials. The structures of target products were confirmed by 1 H NMR, I3 C NMR and HRMS. 2,4,6-Trisubstituted pyrimidine derivatives bearing chalcone moiety were evaluated for anticancer activity on four human cancer cell lines including EC-109, MGC-803, HepG-2 and MDA-MB-231 by CCK-8 (cell counting Kit-8) assay. Among them, (E)-1-(4-((2-(((1H-benzo[d]imidazol-2-yl)methyl)thio)-6-methylpyrimidin-4-yl)amino)phenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one (13u) were more cytotoxic against MGC-803 and MDA-MB-231 cell lines, with IC 50 values of 0.99 and 1.77 μmol•L-1 , respectively.