The synthesis of novel melphalan derivatives as potential antineoplastic agents

Summary Five derivatives of melphalan (( S )-4-[bis(2-chloroethyl)amino]phenylalanine), an alkylating agent presently employed as an antineoplastic in humans, were designed and synthesised as potential prodrugs. Their antitumour activity was tested against P388 leukaemia in mouse after acute intraperitoneal or oral administration and compared with that of the parent compound.