In order to discover novel high efficiency and low toxic anticancer drugs, a series of novel 2-amino-5-ethylpyrimidine derivatives (XIIa-x) were designed and synthesized. Their antiproliferative activities against four human cancer cells were evaluated by MTT assay. Among the synthetic target compounds, the compound 5-ethyl-6-((4-methoxybenzyl)thio)-N-4-(3,4,5-trimethoxyphenyl)pyrimidine-2,4-diamine (XIIw) showed the most potent antiproliferative activity against MGC-803 (human gastric cancer cells), with the IC50 values of 1.02 +/- 0.16 mu M. Meanwhile, this compound inhibited colony formation of MGC-803 cells. Furthermore, this compound blocked the cell cycle in S phase and induced cell apoptosis. Collectively, our findings indicated that this compound was a valuable lead compound to design new anticancer drugs.
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