Abstract
Replacement of the 1-methylimidazol-5-yl moiety in the farnesyltransferase inhibitor ZARNESTRA series by a 4-methyl-1,2,4-triazol-3-yl group gave us compounds with similar structure-activity relationship profiles showing that this triazole is potentially a good surrogate to imidazole for farnesyltransferase inhibition.
MeSH terms
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Administration, Oral
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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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Cell Division / drug effects
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Enzyme Inhibitors / administration & dosage
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology
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Farnesyltranstransferase
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Heterocyclic Compounds / administration & dosage
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Heterocyclic Compounds / chemical synthesis*
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Heterocyclic Compounds / chemistry
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Heterocyclic Compounds / pharmacology
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Humans
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Kinetics
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Mice
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Microsomes, Liver / drug effects
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Microsomes, Liver / metabolism
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Models, Molecular
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Molecular Conformation
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Quinolones / administration & dosage
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Quinolones / chemical synthesis*
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Quinolones / pharmacology*
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Structure-Activity Relationship
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Triazoles / chemical synthesis*
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Triazoles / chemistry
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Triazoles / pharmacology
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Heterocyclic Compounds
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Quinolones
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Triazoles
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Alkyl and Aryl Transferases
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Farnesyltranstransferase
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tipifarnib