Comparative studies on the antitumor activity and the bone marrow toxicity of 1-(beta-D-glucopyranosyl)-3-(2-chloroethyl)-3-nitrosourea and 2-(3-(2-chloroethyl)-3-nitrosoureido)-D-glucopyranose.

Antitumor activity and bone marrow toxicity of a new nitrosourea analog, 1-(beta-D-glucopyranosyl)-3-(2-chloroethyl)-3-nitrosourea (GANU), were compared with those of 2-(3-(2-chloroethyl)-3-nitrosoureido)-D-glucopyranose (Chlorozotocin) and 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU). GANU was found to be highly active against mouse leukemia L-1210 when administered intraperitoneally or intravenously, being the same degree as Chlorozotocin. Even by oral route, GANU exhibited significant activities, whereas Chlorozotocin failed to show any activities by this route. Studies on the bone marrow toxicity as measured by the depression of white blood cell counts and the marrow cellularity revealed that both GANU and Chlorozotocin were less toxic than BCNU. GANU, however, weemed to be rather more toxic than Chlorotocin.