Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0598934 (tumor growth)
 58,965 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Chlorozotocin, 2-(3-(2-chloroethyl)-3-nitrosoureido)-D-glucopyranose, is a newly synthesized, water-soluble nitrosourea antitumor agent that is active against L1210 leukemia in mice. A 701% and a 401% increase in life-span were attained with a dose that was lethal to 10% of the animals (15 to 20 mg/kg, i.p.) in mice treated on Day 2 or Day 6 of L1210 tumor growth, respectivley. Sixity % of Day 2-treated mice and 30% of Day 6-treated mice survived for 90 days. At the maximally effective dose against L1210, chlorozotocin produced no significant depression in normal bone marrow DNA synthesis nor in peripheral neutrophil count, in contrast to a sustained greater than 90% inhibition in L1210 ascites cell DNA synthesis. If the antitumor activity and reduced bone marrow toxicity of chlorozotocin are confirmed in man the use of this compound would facilitate treatment of patients with neoplastic disease who have preexisting abnormal bone marrow function or would allow for the more effective use of a nitrosourea agent in combination with anticancer agents possessing more potent myelosuppressive properties.
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PMID:Chlorozotocin, 2-(3-(2-chloroethyl)-3-nitrosoureido)-D-glucopyranose, an antitumor agent with modified bone marrow toxicity. 12 70

A study was conducted to evaluate the antitumor activities of six nitrosourea derivatives against the xenograft of mammary breast carcinoma transplanted in nude mice (MX-1). 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-deoxyl-D-glucopyranose (DCNU, chlorozotocin). CCNU and Me-CCNU were administered intraperitoneally, and the other were given intravenously 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, we employed the predetermined dose lethal to one-tenth of BDF1 mice (LD10) for each drug as a standard therapeutic dose to nude mice; doses higher than LD10 and one-half and/or one-fourth of LD10 were also given. The results suggest that LD10 in BDF1 mice could be employed as a standard therapeutic dose in the chemotherapy of nude mice.
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PMID:Comparison of antitumor activities of nitrosourea derivatives against mammary breast carcinoma (MX-1) in nude mice. 722 17