Synthesis and preliminary in vitro evaluation of antitumor nitrosoureido cholesterol derivatives

A new class of chloroethyl nitrosourea analogues of cholesterol has been synthetized from the corresponding 7-amino and 7-aminoalkylcholesterol derivatives. Compounds III-V inhibited L1210 cell growth in culture much more effectively than N,N'-bis(2-chloroethyl)-N'-nitrosourea (BCNU) after 48 h incubation. Stability and cytotoxic activity of these prodrugs are promising for brain tumor treatments and as lymphotropic vectors for tumor cells spreading along the lymphatic pathways.