Oxo-piperazine derivatives of N-arylpiperazinones as inhibitors of farnesyltransferase.

Dinsmore, C J; Bergman, J M; Wei, D D; Zartman, C B; Davide, J P; Greenberg, I B; Liu, D; O'Neill, T J; Gibbs, J B; Koblan, K S; Kohl, N E; Lobell, R B; Chen, I W; McLoughlin, D A; Olah, T V; Graham, S L; Hartman, G D; Williams, T M

Dinsmore, C J; Bergman, J M; Wei, D D; Zartman, C B; Davide, J P; Greenberg, I B; Liu, D; O'Neill, T J; Gibbs, J B; Koblan, K S; Kohl, N E; Lobell, R B; Chen, I W; McLoughlin, D A; Olah, T V; Graham, S L; Hartman, G D; Williams, T M.

Affiliation

Dinsmore CJ; Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. christopher_dinsmore@merck.com

Bioorg Med Chem Lett ; 11(4): 537-40, 2001 Feb 26.

Article in En | MEDLINE | ID: mdl-11229765

ABSTRACT

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.

Subject(s)

Alkyl and Aryl Transferases/antagonists & inhibitors; Enzyme Inhibitors/pharmacology; Piperazines/pharmacology; Animals; Dogs; Enzyme Inhibitors/pharmacokinetics; Farnesyltranstransferase; Structure-Activity Relationship

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Collection: 01-internacional Database: MEDLINE Main subject: Piperazines / Alkyl and Aryl Transferases / Enzyme Inhibitors Limits: Animals Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2001 Document type: Article Affiliation country: United States Country of publication: United kingdom

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