Abstract
SDZ 62-434 (CAS 115621-95-9, 5-(4'-piperidinomethylphenyl)-2,3-dihydroimidazo [2,1-a]isoquinoline dihydrochloride), a member of a novel class of antitumor agents, exhibited direct and macrophage-induced cytotoxicity against a variety of murine tumor cell lines. It is more effective than edelfosine in increasing survivors and reducing tumor volume in the oral mouse Meth A fibrosarcoma model. Preliminary studies suggest that an undefined cytotoxic effect, macrophage activation and possible effects on signal transduction may account for its antitumor mechanism of action. SDZ 62-434 is currently in Phase I clinical trials as a potential antitumor agent.
MeSH terms
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Allantoin / metabolism
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Animals
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / toxicity
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Bronchodilator Agents / pharmacology
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Cell Survival / drug effects
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Chick Embryo
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Dogs
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Drug Screening Assays, Antitumor
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Fibroblasts / drug effects
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Fibroblasts / metabolism
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Guinea Pigs
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Hemodynamics / drug effects
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Hemolysis / drug effects
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Humans
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Imidazoles / pharmacology*
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Imidazoles / toxicity
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In Vitro Techniques
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Isoquinolines / pharmacology*
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Isoquinolines / toxicity
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Macrophage Activation / drug effects
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Male
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Mice
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Mice, Inbred Strains
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Neoplasm Transplantation
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Platelet Aggregation / drug effects
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Rats
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Rats, Sprague-Dawley
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Signal Transduction / drug effects
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Bronchodilator Agents
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Imidazoles
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Isoquinolines
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SDZ 62-434
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Allantoin