Analogues of hexamethylmelamine. The anti-neoplastic activity of derivatives with enhanced water solubility.
The preparation of some water soluble analogues of the tumour growth inhibitory hexamethylmelamine is described. The ultra-violet absorption characteristics, solubility and n-octanol/water partition coefficients of these new derivatives and some related compounds have been determined. Rates of demethylation by a liver microsomal preparation and anti-tumour assays against the ADJ/PC6A mouse plasma cell tumour and a human lung tumour xenograft are reported. Two of the derivatives, pentamethylmelamine and N2, N4, N6-trimethyl-N2, N4, N6-trimethylolmelamine, which have shown activity against the xenograft are potential candidates for clinical trials using the intravenous route of administration.
D006585:Altretamine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000627:therapeutic use; D000818:Animals; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy; D051379:Mice; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000188:drug therapy; D010954:Plasmacytoma / Q000188:drug therapy; D012995:Solubility; D013329:Structure-Activity Relationship; D014183:Transplantation, Heterologous; D014227:Triazines / Q000138:chemical synthesis*
D014227:Triazines; D006585:Altretamine