Design, synthesis and antitumor activity evaluation of tetrasubstituted pyrimidine derivatives containing methyl phenyl sulfone group

A series of tetrasubstituted pyrimidine derivatives containing methyl phenyl sulfone structure were designed, synthesized and evaluated for antiproliferative activity against four human cancer cell lines of MGC-803, Eca-109, PC-3 and MCF-7 using methyl thiazolyl tetrazolium (MTT) assay. Most of the compounds displayed moderate to excellent antiproliferative activity against the four human tumor cell lines, among which the compound 27g showed the best antiproliferative activity on MGC-803 cells, with IC 50 value of (2.98 ± 0.13) μM, which is significantly better than that of the positive control 5-FU. Further studies on the anti-tumor mechanism showed that compound 27g significantly inhibited colony formation and migration of MGC-803 cells, blocked the cell cycle in GO/G1 phase, and induced apoptosis. Graphical Abstract