Synthesis and antitumor evaluation of some nitrosourea and nitrogen mustard amino acid derivatives

A series of (2-chloroethyl)nitrosourea and nitrogen mustard amino acid derivatives have been synthesized for antitumor evaluation. Reaction of an appropriate N-protected amino acid with 2-chloroethylamine followed by removal of the N-protecting group and condensation with an active (2-chloroethyl)nitrosocarbamate yielded N-[(2-chloroethyl)nitrosocarbamoyl]amino acid (2-chloroethyl)amides. Antitumor evaluation was performed against leukemia L1210, in vivo, in mice. These derivatives exhibited very interesting activities, particularly the sarcosine and gamma-aminobutyric acid derivatives.