Analogues of hexamethylmelamine. The anti-neoplastic activity of derivatives with enhanced water solubility

Chem Biol Interact. 1977 Jun;17(3):349-57. doi: 10.1016/0009-2797(77)90097-7.

Abstract

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.

MeSH terms

  • Altretamine / analogs & derivatives
  • Altretamine / chemical synthesis*
  • Altretamine / therapeutic use
  • Animals
  • Humans
  • Lung Neoplasms / drug therapy
  • Mice
  • Neoplasm Transplantation
  • Neoplasms, Experimental / drug therapy
  • Plasmacytoma / drug therapy
  • Solubility
  • Structure-Activity Relationship
  • Transplantation, Heterologous
  • Triazines / chemical synthesis*

Substances

  • Triazines
  • Altretamine