N-Diazoacetyl derivatives of glycine and phenylalanine show antitumor activity in mice bearing P388 leukemia or B16 melanoma. The presented data indicate that antitumor activity is shown by diazomethylamide derivatives of glycine and phenylalanine, in addition to that already established for the amino acid derivatives having an O-diazoacetyl group (azaserine) or a diazoketone structure (DON and azotomycin) and for 1,2-bis-diazoacetyl ethane.