2-Substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase

…, TM Ciccarone, SC MacTough, RL Bock…

文献索引：Williams; Ciccarone; MacTough; Bock; Conner; Davide; Hamilton; Koblan; Kohl; Kral; Mosser; Omer; Pompliano; Rands; Schaber; Shah; Wilson; Gibbs; Graham; et al. Journal of Medicinal Chemistry, 1996 , vol. 39, # 7 p. 1345 - 1348

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被引用次数: 71

摘要

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 tetrapeptide, a region of the molecule referred to as the “CaaX box”(C) cysteine, a) any aliphatic amino acid, X) a prenylation specificity residue). 2 The enzyme ...