Abstract
We have identified the pyrazolo[3,4-d]pyrimidine A-420983 (compound 7) as a potent inhibitor of lck. A-420983 exhibits oral efficacy in animal models of delayed-type hypersensitivity and organ transplant rejection.
MeSH terms
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Administration, Oral
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Animals
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Dogs
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Graft Rejection / drug therapy*
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Heart Transplantation / adverse effects
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Humans
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Hypersensitivity, Delayed / drug therapy
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Immunosuppressive Agents / chemical synthesis*
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Immunosuppressive Agents / pharmacokinetics
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Immunosuppressive Agents / therapeutic use
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Inhibitory Concentration 50
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Interleukin-2 / biosynthesis
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Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / antagonists & inhibitors*
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Mice
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Mice, Inbred C57BL
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Microsomes, Liver
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Models, Animal
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Models, Molecular
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Molecular Structure
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Pyrazoles / administration & dosage
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Pyrazoles / pharmacokinetics
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Pyrazoles / therapeutic use*
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Pyrimidines / administration & dosage
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Pyrimidines / pharmacokinetics
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Pyrimidines / therapeutic use*
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Structure-Activity Relationship
Substances
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Immunosuppressive Agents
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Interleukin-2
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Pyrazoles
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Pyrimidines
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pyrazolo(3,4-d)pyrimidine
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Lymphocyte Specific Protein Tyrosine Kinase p56(lck)