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Antitumor activity of halogen analogs of phosphoramide, isophosphoramide, and triphosphoramide mustards, the cytotoxic metabolites of cyclophosphamide, ifosfamide, and trofosfamide
- Source :
- Cancer chemotherapy and pharmacology. 34(3)
- Publication Year :
- 1994
-
Abstract
- A series of halogen analogs of phosphoramide mustard, isophosphoramide mustard, and triphosphoramide mustard, the cytotoxic metabolites of the antitumor drugs cyclophosphamide, ifosfamide, and trofosfamide, respectively, was evaluated in vitro against human tumor cell lines and in vivo against experimental tumors to investigate the effect of replacement of chlorine with bromine or fluorine on the antitumor activity of the parent phosphoramide mustards. In the experimental tumors L1210 leukemia, B16 melanoma, mammary adenocarcinoma 16/C, and ovarian sarcoma M5076, the antitumor activity of the analogs was observed to be generally comparable with that of the parent mustards when chlorine was replaced by bromine but uniformly lower when chlorine was replaced by fluorine. Furthermore, the monobromo analog of isophosphoramide mustard displayed equal or somewhat greater activity in comparison with cyclophosphamide when evaluated against subcutaneously implanted L1210 leukemia with intraperitoneal drug treatment and against mammary adenocarcinoma 16/C.
- Subjects :
- Cancer Research
Cyclophosphamide
chemistry.chemical_element
Antineoplastic Agents
Pharmacology
Toxicology
chemistry.chemical_compound
Mice
In vivo
medicine
Chlorine
Tumor Cells, Cultured
Cytotoxic T cell
Animals
Humans
Pharmacology (medical)
Ifosfamide
Leukemia L1210
Mice, Inbred BALB C
Chemistry
Phosphoramide Mustard
In vitro
Trofosfamide
Oncology
Biochemistry
Mice, Inbred DBA
Phosphoramide Mustards
Drug Screening Assays, Antitumor
medicine.drug
Subjects
Details
- ISSN :
- 03445704
- Volume :
- 34
- Issue :
- 3
- Database :
- OpenAIRE
- Journal :
- Cancer chemotherapy and pharmacology
- Accession number :
- edsair.doi.dedup.....52db99824ed4eacd098b2d9807c70530