Abstract
Farnesyltransferase inhibitors (FTIs) have been developed as potential anti-cancer agents due to their efficacy in blocking malignant growth in a variety of murine models of human tumors. To that end, we have developed a series of pyridone farnesyltransferase inhibitors with potent in vitro and cellular activity. The synthesis, SAR and biological properties of these compounds will be discussed.
MeSH terms
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Alkyl and Aryl Transferases / antagonists & inhibitors*
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / toxicity
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Cell Division / drug effects
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Cell Line, Tumor
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / toxicity
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Farnesyltranstransferase
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Humans
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Molecular Structure
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Pyridones / chemical synthesis*
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Pyridones / pharmacology*
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Pyridones
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Alkyl and Aryl Transferases
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Farnesyltranstransferase