Abstract
Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anti-cancer agents. Analogs of the potent FTI, 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole, were synthesized and tested in vitro for their inhibitory activities. The most promising compound identified from this series is analog 29 that possesses potent 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 / chemistry
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Antineoplastic Agents / pharmacokinetics
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Antineoplastic Agents / pharmacology
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Biological Availability
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Biphenyl Compounds / chemical synthesis*
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Biphenyl Compounds / chemistry
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Biphenyl Compounds / pharmacokinetics
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Biphenyl Compounds / pharmacology
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Farnesyltranstransferase
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacokinetics
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Imidazoles / pharmacology
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In Vitro Techniques
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Rats
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Structure-Activity Relationship
Substances
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1-benzyl-5-(3-biphenyl-2-ylpropyl)-1H-imidazole
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Antineoplastic Agents
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Biphenyl Compounds
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Imidazoles
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Alkyl and Aryl Transferases
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geranylgeranyltransferase type-I
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Farnesyltranstransferase