In vitro cytotoxicity of the methylmelamines.
Hexamethylmelamine (HMM) and a number of its derivatives are toxic to PC6 plasmacytoma cells in vitro. However, there is no correlation between in vitro cytotoxicity and activity against this tumour in vivo. N-Methylolmelamines are significantly more toxic than HMM itself. These compounds break down to release formaldehyde which is itself a highly cytotoxic agent. Pentamethylmonomethylolmelamine rapidly inhibits the growth of PC6 cells in culture, whereas HMM and pentamethylmelamine (PMM) require prolonged contact with the cells in order to exert a cytotoxic effect. HMM and its metabolites are also toxic to a number of other cell lines. The toxicity of the N-methylols to cultured L1210 leukaemia and Walker 256 ascites cells appears to be due entirely to formaldehyde release, whereas in PC6 cells the methylols appear to be acting more selectively.
D006585:Altretamine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology*; D000818:Animals; D002470:Cell Survival / Q000187:drug effects*; D002478:Cells, Cultured; D005557:Formaldehyde / Q000378:metabolism; D051379:Mice; D009374:Neoplasms, Experimental / Q000188:drug therapy* / Q000378:metabolism; D012663:Semicarbazides / Q000494:pharmacology; D014227:Triazines / Q000031:analogs & derivatives* / Q000494:pharmacology*
D012663:Semicarbazides; D014227:Triazines; C024065:pentamethylmonomethylolmelamine; D005557:Formaldehyde; D006585:Altretamine; C022048:pentamethylmelamine