Abstract
A structure-activity study was performed by synthesis on N,N'-disubstitution of 3-aminobenzo[c] and [d]azepin-2-one 2 and 3 to afford potent and specific farnesyl transferase inhibitors with low nM enzymatic and cellular activities.
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 / pharmacology
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Azepines / chemical synthesis*
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Azepines / pharmacology*
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Caco-2 Cells / drug effects
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Caco-2 Cells / enzymology
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Cell Line, Transformed / transplantation
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Drug Screening Assays, Antitumor
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology
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Farnesyltranstransferase
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Genes, ras
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Humans
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Inhibitory Concentration 50
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Mice
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Mice, Nude
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Molecular Structure
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Protein Conformation / drug effects
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Rats
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Structure-Activity Relationship
Substances
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Antineoplastic Agents
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Azepines
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Enzyme Inhibitors
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Alkyl and Aryl Transferases
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geranylgeranyltransferase type-I
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Farnesyltranstransferase