Abstract
Farnesyltransferase inhibitors (FTIs) have emerged as a novel class of anticancer 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 most promising compound identified from this series is analogue 11 that possesses potent enzymatic and cellular activities.
MeSH terms
-
3T3 Cells
-
Alkyl and Aryl Transferases / antagonists & inhibitors*
-
Animals
-
Antineoplastic Agents / chemical synthesis*
-
Antineoplastic Agents / pharmacology*
-
Enzyme Inhibitors / chemical synthesis*
-
Enzyme Inhibitors / pharmacology*
-
Farnesyltranstransferase
-
Imidazoles / chemical synthesis*
-
Imidazoles / pharmacology*
-
Indicators and Reagents
-
Mice
-
Nitriles / chemical synthesis*
-
Nitriles / pharmacology*
-
Structure-Activity Relationship
-
gamma-Glutamyltransferase / antagonists & inhibitors
Substances
-
4-((3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl)-benzonitrile
-
Antineoplastic Agents
-
Enzyme Inhibitors
-
Imidazoles
-
Indicators and Reagents
-
Nitriles
-
gamma-Glutamyltransferase
-
Alkyl and Aryl Transferases
-
geranylgeranyltransferase type-I
-
Farnesyltranstransferase