Abstract
The synthesis and evaluation of farnesyl-derived inhibitors of ras farnesyl transferase are presented. Evaluation of inhibitors of farnesyl transferase and comparison with the previously described inhibitor was accomplished using purified enzyme and Amersham′s Farnesyl:Transferase enzyme assay kit. These results show an order of magnitude increase in inhibitory activity for β-ketophosphonic acid over β-hydroxyphosphonic acid. Incorporation of fluorines in α-position, led to an increase in inhibitory activity over the nonfluorinated analogues.
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Schedule a callMore From: Biochemical and biophysical research communications
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