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A series of N-methyl, N-(2-chloroethyl) and N-propargyl urea and nitrosourea derivatives of amino acids were synthesized and tested for anti-HIV and anti-proliferative activity. All the agents tested showed only a weak activity to counteract the cytopathic effects of the HIV-1 virus on a T4 lymphocyte cell line (CEM-IW). At high concentration, the N-methyl and N-propargyl ureas were cytotoxic. The nitrosoureas failed to suppress cell proliferation of uninfected CEM-IW cells. The lack of activity and cytotoxicity of the nitrosoureas in this model could be explained by their short chemical half-life.

Synthesis, anti-HIV and anti-Proliferative Activity of New Urea and Nitrosourea Derivatives of Amino Acids