Abstract
Synthesis and biological evaluation of various colchicine analogues through the mixed-lymphocyte reaction (MLR), lymphoproliferation, and inhibitory effects on the inflammatory genes are described. In addition, a new series of immunosuppressive agents developed on the structural basis of colchicine, as well as their structure-activity relationships is reported. The most potent analogue 20a exhibited an excellent immunosuppressive activity on in vivo skin-allograft model, which is comparable to that of cyclosporin A.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Autoimmune Diseases / drug therapy
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Chemistry, Pharmaceutical / methods
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Colchicine / analogs & derivatives*
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Colchicine / chemical synthesis
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Colchicine / pharmacology
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Cyclosporine / pharmacology
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Drug Design
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Gout Suppressants / chemical synthesis
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Gout Suppressants / pharmacology
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Graft Rejection
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Humans
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Immunosuppressive Agents / chemical synthesis*
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Immunosuppressive Agents / pharmacology
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Inflammation
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Inhibitory Concentration 50
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Mice
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Mice, Inbred BALB C
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Mice, Inbred C57BL
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Rats
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Skin Transplantation
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Structure-Activity Relationship
Substances
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Gout Suppressants
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Immunosuppressive Agents
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Cyclosporine
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Colchicine