In vitro cytotoxicity of imidazolyl-1,3,5-triazine derivatives.
We examined in vitro cytotoxic activity of imidazolyl-1,3,5-triazine derivatives using human breast cancer cell lines (MCF-7, R-27, T-47D and ZR-75-1) and murine leukemia cell line (P388). The percentage of viable cells was determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazorium bromide (MTT) assay. Hexamethylmelamine (HMM), a 1,3,5-triazine derivative has previously been recognized as an antitumor agent effective against lung, ovarian and breast cancer, but failed to show a significant cytotoxic activity in the present study. In contrast, four imidazolyl-1,3,5-triazine derivatives, 2-(1-imidazolyl)-4,6-bis(morpholino)-1,3,5-triazine, 2-(1-imidazolyl)-4-morpholino-6-(3-thiazolidinyl)-1,3,5-triazine, 2-(4-cyano-4-phenylpiperidino)-4-(1-imidazolyl)-6-morpholino-1,3,5-triaz ine and 2-(1-imidazolyl)-4-(N-methyl-N-phenylamino)-6-morpholino-1,3,5-triazine showed cytotoxic activity for most cell lines, which was significantly greater than the activity of hydroxymethylpentamethylmelamine (HMPMM), a major metabolite of HMM.
Yaguchi
S
S
Research Laboratory, Zenyaku Kogyo Co., Ltd., Tokyo, Japan.
Izumisawa
Y
Y
Sato
M
M
Nakagane
T
T
Koshimizu
I
I
Sakita
K
K
Kato
M
M
Yoshioka
K
K
Sakato
M
M
Kawashima
S
S
D006585:Altretamine / Q000031:analogs & derivatives / Q000494:pharmacology; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000473:pathology; D002470:Cell Survival / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D017316:Fadrozole / Q000494:pharmacology; D006801:Humans; D007941:Leukemia P388 / Q000473:pathology; D051379:Mice; D013329:Structure-Activity Relationship; D014227:Triazines / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D014227:Triazines; C081888:2-N,N-dimethylamino-4,6-bis(1-H-imidazol-1-yl)-1,3,5-triazine; D017316:Fadrozole; D006585:Altretamine