The isomeric intermediates, $3{alpha}$and $3{eta}-amino-5{alpha}-cholestane required for the synthesis of N-nitrosoureas, N-(2-chloroethyl)-N-nitrosocarbamoyl-$3{alpha}-amino-5{alpha}$-cholestane (9), N-methyl-N-nitrosocarbamoyl-3${alpha}-amino-5{alpha}-cholestane$ (10), N-(2-chloroethyl)-N-nitrosocarbamoyl-$3{eta}-amino-5{alpha}-cholestane$: (7), and N-methyl-N-nitrosocarbamoyl-$3{eta}-amino-5{alpha}-cholestane$ (8) were obtained through the $LiAlH_{4}$ reduction of $5{alpha}$-cholestan-3-one oxime, followed by the chromatographic separation: the assignment of the stereochemistry of both isomers were based on the shape and chemical shift of $C_{3}$-proton resonances on their NMR spectra and on the elution mobility on the TLC. The urea intermediates, N-(2-chloroethyl) carbamoyl-3.alpha.-amino-5.alpha.-cholestane (13), N-methylcarbamoyl-$3{alpha}-amino-5{alpha}-cholestane$ (14), N-(2-chloroethyl) carbamoyl-$3{eta}-amino-5{alpha}-cholestane (11) and N-methyl-$3{eta}-amino-5{alpha}$-cholestane (12) were prepared by the treatment of each isomers ($3{alpha}$-amino-and $3{eta}-amino-5{alpha}$-cholestane) with alkyl isocyanates in anhydrous $CHCl_{3}$, and the corresponding nitrosoureas, 7-10 were obtained by the nitrosation of the ureas, 11-14, with AcOH (or HCOOH)/$NaNO_{2}$ in ice-cold condition. The inhibitory activity of the nitrosoureas, 7-10, and their intermediates, 12-14 towards the growth of L1210 murine leukemia cells, were examined. Among them, the compounds 9 and 10 exhibited high activity having $ED_{50}$ to be 5.5g/ml and 6.1g/ml, respectively.