We examined in vitro cytotoxic activity of imidazolyl-1,3,5-triazine d
erivatives using human breast cancer cell lines (MCF-7, R-27, T-47D an
d ZR-75-1) and murine leukemia cell line (P388). The percentage of via
ble cells was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphe
ny tetrazorium bromide (MTT) assay. Hexamethylmelamine (HMM), a 1,3,5-
triazine derivative has previously been recognized as an antitumor age
nt effective against lung, ovarian and breast cancer, but failed to sh
ow a significant cytotoxic activity in the present study. In contrast,
four imidazolyl-1,3,5-triazine derivatives, (1-imidazolyl)-4,6-bis(mo
rpholino)-1,3,5-triazine, )-1-morpholino-6-(3-thiazolidinyl)-1,3,5-tri
azine, dino)-4-(1-imidazolyl)-6-morpholino-1,3,5-triazine and azolyl)-
4-(N-methyl-N-phenylamino)-6-morpholino-1, 3,5-triazine showed cytotox
ic activity for most cell lines, which was significantly greater than
the activity of hydroxymethylpentamethylmelamine (HMPMM), a major meta
bolite of HMM.