Oxo-piperazine Derivatives of N-Arylpiperazinones as Inhibitors of Farnesyltransferase

Oxo-piperazine Derivatives of N-Arylpiperazinones as Inhibitors of Farnesyltransferase

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 pharmacokinetic profile relative to the parent 1-ary...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2001-02, Vol.11 (4), p.537-540
Hauptverfasser: Dinsmore, Christopher J, Bergman, Jeffrey M, Wei, Donna D, Zartman, C.Blair, 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
Format: Artikel
Sprache:eng
Schlagworte:
Alkyl and Aryl Transferases - antagonists & inhibitors
Animals
Antineoplastic agents
Biological and medical sciences
Dogs
Enzyme Inhibitors - pharmacokinetics
Enzyme Inhibitors - pharmacology
Farnesyltranstransferase
General aspects
Medical sciences
Pharmacology. Drug treatments
Piperazines - pharmacology
Structure-Activity Relationship
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Zusammenfassung: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 pharmacokinetic profile relative to the parent 1-aryl-2-piperazinones. Graphic
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(00)00710-1