Abstract
A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, Non-P.H.S.
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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Biological Availability
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Crystallography, X-Ray
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Dogs
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Drug Design
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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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Haplorhini
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology
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Models, Molecular
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Nitriles / chemical synthesis*
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Nitriles / chemistry
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Nitriles / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Imidazoles
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Nitriles
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Alkyl and Aryl Transferases
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Farnesyltranstransferase