PMID- 6510639 OWN - NLM STAT- MEDLINE DCOM- 19850204 LR - 20141003 IS - 0016-450X (Print) IS - 0016-450X (Linking) VI - 75 IP - 10 DP - 1984 Oct TI - Antitumor activity and toxicity of methyl 6-[3-(2-chloroethyl)- 3-nitrosoureido]-6-deoxy-alpha-D-glucopyranoside in experimental animals. PG - 937-46 AB - A new water-soluble nitrosourea derivative, methyl 6-[3-(2-chloroethyl)-3-nitrosoureido]-6-deoxy-alpha-D-glucopyranoside (MCNU), was tested for antitumor activity against murine tumors (L1210 and P388 leukemias, B16 melanoma, and Lewis lung carcinoma) and BC-47 rat bladder carcinoma, and the results were compared with those for four other nitrosourea derivatives; chlorozotocin, 1-(2-chloroethyl)-3-(beta-D-glucopyranosyl)-1-nitrosourea (GANU), 3-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-1-(2-chloroethyl)-1- nitrosourea hydrochloride (ACNU), and 1-(2-chloroethyl)-3-(4-methylcyclohexyl)-1-nitrosourea (methyl-CCNU). MCNU was shown not only to have a broad antitumor spectrum against all the tumors tested, but also to be effective over a wide range of dosages. The antitumor activity of MCNU was superior to those of GANU and chlorozotocin and similar to those of ACNU and methyl-CCNU. Furthermore, MCNU and other nitrosoureas were evaluated for toxicity in BDF1 female mice with respect to body weight changes. Weight loss in mice given MCNU at a dose lethal to 10% of the mice was relatively mild and the treated mice regained body weight most rapidly to the pretreatment level among all groups receiving the above drugs at equitoxic doses. These results may suggest that MCNU is a new nitrosourea derivative worthwhile to perform clinical trials. FAU - Fujimoto, S AU - Fujimoto S FAU - Tashiro, T AU - Tashiro T FAU - Ogawa, M AU - Ogawa M LA - eng PT - Comparative Study PT - Journal Article PL - Japan TA - Gan JT - Gan JID - 0151745 RN - 0 (Antineoplastic Agents) RN - 0 (Nitrosourea Compounds) RN - RYH2T97J77 (ranimustine) SB - IM MH - Animals MH - Antineoplastic Agents/*therapeutic use MH - Cell Line MH - Leukemia L1210/drug therapy MH - Leukemia P388/drug therapy MH - Lung Neoplasms/drug therapy MH - Melanoma/drug therapy MH - Mice MH - Neoplasms, Experimental/*drug therapy MH - Nitrosourea Compounds/*therapeutic use/toxicity MH - Structure-Activity Relationship MH - Tumor Stem Cell Assay MH - Urinary Bladder Neoplasms/drug therapy EDAT- 1984/10/01 00:00 MHDA- 1984/10/01 00:01 CRDT- 1984/10/01 00:00 PHST- 1984/10/01 00:00 [pubmed] PHST- 1984/10/01 00:01 [medline] PHST- 1984/10/01 00:00 [entrez] PST - ppublish SO - Gan. 1984 Oct;75(10):937-46.