2-Substituted Piperazines as Constrained Amino Acids. Application to the Synthesis of Potent, Non Carboxylic Acid Inhibitors of Farnesyltransferase (original) (raw)

Journal of Medicinal Chemistry, 1996

Charles Omer

Michael Conner

Samuel Graham

Kelly Hamilton

Astrid Kral

Daksha Shah

J. Gibbs

Robert Smith

Abstract

Mutations in the ras oncogene are present in many human cancers, including 30−50% of colon and 90% of pancreatic cancer. 1,2 The Ras protein undergoes a series of post-translational modifications, including S-farnesylation of a cysteine residue located in the C-terminal ...

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