186203-16-7Relevant academic research and scientific papers
Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase
Dinsmore, Christopher J,Bergman, Jeffrey M,Wei, Donna D,Zartman,Davide, Joseph P,Greenberg, Ian B,Liu, Dongming,O'Neill, Timothy J,Gibbs, Jackson B,Koblan, Kenneth S,Kohl, Nancy E,Lobell, Robert B,Chen, I-Wu,McLoughlin, Debra A,Olah, Timothy V,Graham, Samuel L,Hartman, George D,Williams, Theresa M
, p. 537 - 540 (2007/10/03)
The evaluation of SAR associated with the insertion of carbonyl groups at various positions of N-arylpiperazinone farnesyltransferase inhibitors is described herein. 1-Aryl-2,3-diketopiperazine derivatives exhibited the best balance of potency and pharmac
INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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, (2008/06/13)
The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras
INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
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, (2008/06/13)
The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production
