Abstract
A tether length study of C32-O-phenalkyl ether derivatives of ascomycin was conducted wherein it was determined that a 2-carbon tether provides optimum in vitro immunosuppressive activity. Oxygen-bearing substituents along the 2-carbon tether can further increase the potency of this design.
MeSH terms
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Animals
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Cell Division / drug effects
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Drug Design
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Drug Evaluation, Preclinical
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Immunophilins / metabolism
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Immunosuppressive Agents / chemical synthesis*
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Immunosuppressive Agents / metabolism
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Immunosuppressive Agents / pharmacology*
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Inhibitory Concentration 50
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Macrolides / chemical synthesis*
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Macrolides / pharmacology*
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Structure-Activity Relationship
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T-Lymphocytes / drug effects
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Tacrolimus / analogs & derivatives*
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Tacrolimus / chemistry
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Tacrolimus / pharmacology
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Tacrolimus Binding Proteins
Substances
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Immunosuppressive Agents
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Macrolides
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immunomycin
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Tacrolimus Binding Proteins
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Immunophilins
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Tacrolimus