L. Elkihel et al., SYNTHESIS AND PRELIMINARY IN-VITRO EVALUATION OF ANTITUMOR NITROSOUREIDO CHOLESTEROL DERIVATIVES, Arzneimittel-Forschung, 45-1(2), 1995, pp. 190-194
A new class of chloroethyl nitrosourea analogues of cholesterol has be
en synthetized from the corresponding 7-amino and 7-aminoalkylcholeste
rol derivatives. Compounds III-V inhibited L1210 cell growth in cultur
e much more effecfively than N,N'-bis(2-chloroethyl)-N'-nitrosourea (B
CNU) 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.