Abstract
A modified approach to the synthesis of 3-(oxazolyl-5-yl) indoles is reported. This method was applied to the synthesis of series of novel indole based inhibitors of inosine monophosphate dehydrogenase (IMPDH). The synthesis and the structure-activity relationships (SARs), derived from in vitro studies, for this new series of inhibitors is given.
MeSH terms
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Binding Sites
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Cyanides / chemistry
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacology
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Humans
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IMP Dehydrogenase / antagonists & inhibitors*
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Indoles / chemical synthesis
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Indoles / pharmacology*
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Lymphocyte Activation / drug effects
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Structure-Activity Relationship
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T-Lymphocytes / drug effects
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Tumor Cells, Cultured
Substances
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Cyanides
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Enzyme Inhibitors
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Indoles
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tosylmethyl isocyanide
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IMP Dehydrogenase