Abstract
Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anti-cancer agents. Analogues of the potent FTI, 4-[3-biphenyl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl]-1-yl-benzonitrile, were synthesized and tested in vitro for their inhibitory activities. The synthesis and detailed biological data of this series of analogues are presented.
MeSH terms
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3T3 Cells
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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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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Farnesyltranstransferase
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Genes, ras / drug effects
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacology*
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Mice
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Nitriles / chemical synthesis*
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Nitriles / pharmacology*
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Structure-Activity Relationship
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gamma-Glutamyltransferase / antagonists & inhibitors
Substances
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4-(3-biphenyl-2-yl-1-hydroxy-1-(3-methyl-3H-imidazol-4-yl)-prop-2-ynyl)-1-yl-benzonitrile
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Antineoplastic Agents
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Enzyme Inhibitors
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Imidazoles
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Nitriles
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gamma-Glutamyltransferase
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Alkyl and Aryl Transferases
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Farnesyltranstransferase