COMPARISON OF ANTI-TUMOR ACTIVITIES OF NITROSOUREA DERIVATIVES AGAINST MAMMARY BREAST-CARCINOMA (MX-1) IN NUDE-MICE

  • 1 January 1980
    • journal article
    • research article
    • Vol. 71  (5) , 686-691
Abstract
The antitumor activities of 6 nitrosourea derivatives were evaluated against the xenograft of [human] mammary breast carcinoma MX-1 cells transplanted in nude mice. The drugs employed in this study were 3-[(4-amino-2-methyl-5-pyrimidinyl)methyl]-1-(2-chloroethyl)-1-nitrosourea hydrochloride (ACNU), 1-(2-chloroethyl)-3-(methyl-.alpha.-D-glucopyranos-6-yl)-1-nitrosourea (MCNU), 1-(2-chloroethyl)-3-(.beta.-D-glucopyranosyl)-1-nitrosourea (GANU), 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (CCNU), 1-(2-chloroethyl)-3-(4-methylcyclohexyl)-1-nitrosourea (Me-CCNU) and 2-[3-(2-chloroethyl)-3-nitrosoureido]2-deoxy-D-glucopyranose (DCNU, chlorozotocin). CCNU and Me-CCNU were administered i.p., and the others were given i.v. through a tail vein. Antitumor activities were assessed in terms of the drug-induced tumor growth inhibition based on caliper measurements. A single treatment with ACNU (40 mg/kg) induced 92% tumor regression, compared to 73% and 69% tumor regression induced by MCNU (15 mg/kg) and CCNU (50 mg/kg), respectively. GANU and DCNU were less effective. To evaluate the antitumor activity of the drugs, the predetermined dose lethal to 1/10 of BDF1 mice (LD10) was employed for each drug as a standard therapeutic dose to nude mice; doses higher than LD10 and 1/2 and/or 1/4 of LD10 were also given. LD10 in BDF1 mice probably could be employed as a standard therapeutic dose in the chemotherapy of nude mice.

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