Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.

Terrence M. Ciccarone,Suzanne C. MacTough,Theresa M. Williams,Christopher J. Dinsmore,Timothy J. ONeill,Daksha Shah,J.Christopher Culberson,Kenneth S. Koblan,Nancy E. Kohl,Jackson B. Gibbs,Allen Oliff,Samuel L. Graham,George D. Hartman

Non-thiol 3-aminomethylbenzamide inhibitors of farnesyl-protein transferase.

1999

Terrence M. Ciccarone
Suzanne C. MacTough
Theresa M. Williams
Christopher J. Dinsmore
Timothy J. ONeill
Daksha Shah
J.Christopher Culberson
Kenneth S. Koblan
Nancy E. Kohl
Jackson B. Gibbs
Allen Oliff
Samuel L. Graham
George D. Hartman

The design and syntheses of non-thiol inhibitors of farnesyl-protein transferase are described. Substitutions on an imidazolylmethyl-AMBA-methionine template gave a highly potent and cell-active inhibitor.

Keywords:

Chemical synthesis
Farnesyltranstransferase
Enzyme
Organic chemistry
Thiol
Farnesyl Protein Transferase
Nitrile
Chemistry
Biochemistry
Stereochemistry
Transferase
Enzyme inhibitor
Structure–activity relationship
Binding site

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