(2-Chloroethyl)nitrosourea congeners of amino acid amides

J Med Chem. 1982 Jul;25(7):829-32. doi: 10.1021/jm00349a012.


Fourteen (2-chloroethyl)nitrosourea congeners of L-amino acid amides have been synthesized as potential antineoplastic agents. Almost all the congeners tested were found to be highly active against experimental leukemia L1210 in mice. The chemical decomposition rates of the congeners were measured in a buffered solution (pH 7.4) at 37 degrees C. Acute toxicities of some of the congeners were determined for mice. The congener of sarcosinamide shows the longest half-life (T0.5 = 329.7 min) and the lowest toxicity, LD50 = 392.0 mg/kg (ip) and 426.6 mg/kg (iv), in this series.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acids / chemical synthesis
  • Amino Acids / pharmacology
  • Animals
  • Antineoplastic Agents / chemical synthesis*
  • Chemical Phenomena
  • Chemistry
  • Lethal Dose 50
  • Leukemia L1210 / drug therapy
  • Male
  • Mice
  • Nitrosourea Compounds / chemical synthesis*
  • Nitrosourea Compounds / pharmacology
  • Nitrosourea Compounds / toxicity


  • Amino Acids
  • Antineoplastic Agents
  • Nitrosourea Compounds